Pictilisib (Synonyms: GDC-0941)

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摩尔计算器

Pictilisib (GDC-0941) 是有效的 PI3Kα/δ 抑制剂，IC₅₀为 3 nM；对110β (11倍) 和 p110γ (25倍) 具有适度的选择性。

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Pictilisib Chemical Structure

CAS No. : 957054-30-7

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥735	In-stock
1 mg	￥295	In-stock
5 mg	￥650	In-stock
10 mg	￥850	In-stock
25 mg	￥1379	In-stock
50 mg	￥2000	In-stock
100 mg	￥3200	In-stock
200 mg	￥4500	In-stock
500 mg		询价
1 g		询价

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Customer Review

Other Forms of Pictilisib:

Pictilisib dimethanesulfonate In-stock

MCE 顾客使用本产品发表的 50 篇科研文献

Proliferation Assay

: Pictilisib purchased from MCE. Usage Cited in: Int J Oncol. 2017 Sep;51(3):823-831. [Abstract]; Protein levels of BRD4, p-AKT and AKT in GDC-0941 treated NOZ cells after 72 h.

: Pictilisib purchased from MCE. Usage Cited in: Nat Commun. 2016 Feb 2;7:10438. [Abstract]; Western blot illustrating the effect of PI3K inhibitors on p21 protein levels in MEFs. Cells are treated for 24 hours with the indicated concentrations of the different drugs.

: Pictilisib purchased from MCE. Usage Cited in: Oncogene. 2016 Jun 9;35(23):2961-70. [Abstract]; Western blot analysis of p-AKT(T308), p-AKT(S473) and p-ERK in transplanted NIC⁺PIK3CA^H1047R tumors treated as indicated.

: Pictilisib purchased from MCE. Usage Cited in: Oncotarget. 2016 Aug 16;7(33):53515-53525. [Abstract]; PI3KD/V-IN-01 affects autophagy HeLa cells are treated with different concentrations of PI3KD/V-IN-01, VPS34-IN-1, GDC-0941 or CAL-101 for 16 hours before they are fixed and stained for the autophagy marker LC3B.

: Pictilisib purchased from MCE. Usage Cited in: Oncotarget. 2016 May 31;7(22):32641-51. [Abstract]; The well-established PI3Kδ specific inhibitor, CAL-101, shows similar effects as PI3KD-IN-015 with an EC₅₀ of 2.3 nM against PI3Kδ and over 1000-fold less potent against the other three isoforms. Determination of CAL-101 inhibitory activities against PI3Kα, β, δ and γ in cellular background.

: Pictilisib purchased from MCE. Usage Cited in: Cancer Res. 2014 Jan 1;74(1):15-23. [Abstract]; Differential responses of Pten Lkb1-deficient endometrial tumors to inhibitors targeting PI3K and/or mTOR. Mice bearing transplanted Pten Lkb1-deficient endometrial tumors are treated with indicated drugs for 3 days and sacrificed three hours after their dose on day 3 of treatment; their tumors are isolated and tumor lysates are immunoblotted with the indicated antibodies.

: Pictilisib purchased from MCE. Usage Cited in: Cancer Res. 2014 Jan 1;74(1):15-23. [Abstract]; Ectopic expression of LKB1 renders PTEN LKB1-deficient endometrial cancer cells susceptible to PI3K inhibition. Western blot analysis of pS6RP (Ser235/236) and p4EBP1(Ser65) in ETN-1 and HEC108 cells with stable expression of vector or flag- tagged LKB1. Cell lysates were harvested 24 hours after GDC-0941 treatment.

: Pictilisib purchased from MCE. Usage Cited in: Sci Transl Med. 2013 Jul 31;5(196):196ra99. [Abstract]; Sensitivity to GDC-0941 in parental MDA453 and T47D and BYL719-resistant MDA453R and T47DR cells. Protein lysates are isolated after 24 hours of treatment with 1 μM GDC-0941 and probed against the indicated proteins.

: Pictilisib purchased from MCE. Usage Cited in: Cancer Discov. 2012 May;2(5):425-33. [Abstract]; Effects of KIN-193, GDC-0941, PIK-75 and IC87114 on AKT phosphorylation in PTEN-deficient cell lines as indicated. Representative western blots are shown. Bar graphs represent mean ± SD of western blot quantitations of AKTT308 (n=3).

: Pictilisib purchased from MCE. Usage Cited in: Cell Metab. 2012 Mar 7;15(3):382-94. [Abstract]; Effect of the indicated PI3K inhibitors on pre-brown adipocytes. Cultures are treated with the inhibitors at the indicated concentrations (μM) for 4 h. Protein levels (top) and mRNA levels (bottom) of the indicated proteins and genes, respectively, are analyzed. Assays are performed in triplicate cultures. Values represent mean ± sd, and statistical significance is determined by the two-tailed Student’s t-test. *p<0.05, **p<0.01.

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC₅₀ of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

IC₅₀ & Target^[5]

p110α

3 nM (IC₅₀)

p110α-H1047R

3 nM (IC₅₀)

p110α-E545K

3 nM (IC₅₀)

p110δ

3 nM (IC₅₀)

p110β

33 nM (IC₅₀)

p110γ

75 nM (IC₅₀)

mTOR

0.58 μM (Ki)

DNA-PK

1.23 μM (IC₅₀)

Autophagy

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.14 μM Compound: 17, GDC-0941	Antiproliferative activity against human A2780 cells with PIK3CA and PTEN mutation after 4 days by alamar blue assay Antiproliferative activity against human A2780 cells with PIK3CA and PTEN mutation after 4 days by alamar blue assay	[PMID: 18754654]
A549	IC₅₀	1.03 μM Compound: GDC-0941	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
A549	IC₅₀	1.2 μM Compound: GDC-0941	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27043268]
A549	GI₅₀	1217 nM Compound: 2	Cytotoxicity against ALK-negative human A549 cells harboring wild type PI3KCA and CDKN2A and KRAS mutations assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against ALK-negative human A549 cells harboring wild type PI3KCA and CDKN2A and KRAS mutations assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32184963]
A549	IC₅₀	2.28 μM Compound: GDC0941	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 25911625]
A549	IC₅₀	2.48 μM Compound: GDC-0941	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
A549	IC₅₀	6.9 μM Compound: 1, GDC-0941	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
A549	IC₅₀	6.99 μM Compound: GDC-0941b	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 27353887]
Calu-3	IC₅₀	2.87 μM Compound: GDC-0941	Antiproliferative activity against human Calu3 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human Calu3 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
HCC1954	IC₅₀	1.3 μM Compound: GDC0941	Cytotoxicity against human HCC1954 cells by MTT assay Cytotoxicity against human HCC1954 cells by MTT assay	[PMID: 28006668]
HCT-116	IC₅₀	0.37 μM Compound: GDC0941	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 25911625]
HeLa	IC₅₀	2.97 μM Compound: GDC-0941	Antiproliferative activity against paclitaxel-resistant human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against paclitaxel-resistant human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
HeLa	IC₅₀	3.15 μM Compound: GDC-0941	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
Hep 3B2	IC₅₀	2.03 μM Compound: Pic; GDC-0941	Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
HepG2	IC₅₀	1 μM Compound: 1, GDC-0941	Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
HepG2	IC₅₀	6.22 μM Compound: Pic; GDC-0941	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
HT-29	IC₅₀	0.66 μM Compound: 1, GDC-0941	Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
HT-29	IC₅₀	0.86 μM Compound: 1, GDC-0941	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 25440879]
HT-29	IC₅₀	0.86 μM Compound: 1, GDC-0941	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 25086238]
Huh-7	IC₅₀	1.72 μM Compound: Pic; GDC-0941	Antiproliferative activity against human HuH-7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human HuH-7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
JeKo-1	GI₅₀	5 μM Compound: GDC-0941	Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
K562	IC₅₀	6.34 μM Compound: Pic; GDC-0941	Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
LNCaP	IC₅₀	0.34 μM Compound: 1; GDC-0941	Antiproliferative activity against PTEN deficient human LNCAP cells after 72 hrs by CCK-8 assay Antiproliferative activity against PTEN deficient human LNCAP cells after 72 hrs by CCK-8 assay	[PMID: 28409639]
MCF7	IC₅₀	0.07 μM Compound: GDC-0941b	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 27353887]
MCF7	IC₅₀	0.22 μM Compound: Pic; GDC-0941	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay	[PMID: 29360358]
MCF7	IC₅₀	1.09 μM Compound: GDC0941	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 25911625]
MCF7	IC₅₀	1.2 μM Compound: GDC-0941	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
MCF7	IC₅₀	2 μM Compound: GDC0941	Cytotoxicity against human MCF7 cells by MTT assay Cytotoxicity against human MCF7 cells by MTT assay	[PMID: 28006668]
MCF7	GI₅₀	70.2 nM Compound: GDC-0941	Growth inhibition of human MCF7 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay Growth inhibition of human MCF7 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay	[PMID: 23360348]
MDA-MB-231	IC₅₀	> 30 μM Compound: GDC0941	Cytotoxicity against human MDA-MB-231 cells by MTT assay Cytotoxicity against human MDA-MB-231 cells by MTT assay	[PMID: 28006668]
MDA-MB-231	IC₅₀	0.28 μM Compound: 1, GDC-0941	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 25440879]
MDA-MB-231	IC₅₀	0.28 μM Compound: 1, GDC-0941	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 25086238]
MDA-MB-231	GI₅₀	12 μM Compound: GDC-0941	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MDA-MB-231	IC₅₀	73.82 μM Compound: 1, GDC-0941	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
MDA-MB-361	IC₅₀	0.72 μM Compound: 17, GDC-0941	Antiproliferative activity against human MDA-MB-361 cells with PIK3CA E545-K mutation after 96 hrs by alamar blue assay Antiproliferative activity against human MDA-MB-361 cells with PIK3CA E545-K mutation after 96 hrs by alamar blue assay	[PMID: 18754654]
MIA PaCa-2	GI₅₀	12 μM Compound: GDC-0941	Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MKN-45	IC₅₀	0.6 μM Compound: 1, GDC-0941	Cytotoxicity against human MKN45 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 25440879]
MKN-45	IC₅₀	0.6 μM Compound: 1, GDC-0941	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 25086238]
MM1.S	IC₅₀	0.1 μM Compound: GDC-0941	Antiproliferative activity against human MM1S cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MM1S cells after 72 hrs by CellTiter-Glo assay	[PMID: 30715878]
MOLM-13	GI₅₀	0.048 μM Compound: 16; GDC-0941c	Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
MOLM-14	GI₅₀	0.21 μM Compound: 16; GDC-0941c	Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
MOLT-4	IC₅₀	0.18 μM Compound: Pic; GDC-0941	Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
MV4-11	GI₅₀	0.88 μM Compound: 16; GDC-0941c	Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
MV4-11	IC₅₀	1.46 μM Compound: Pic; GDC-0941	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay	[PMID: 29360358]
MV4-11	EC₅₀	10.7 μM Compound: Pic; GDC-0941	Induction of apoptosis in human MV4-11 cells assessed as increase in caspase 3/7 activity measured at 24 hrs in presence of Z-DEVD-R110 or (Z-Asp-Glu-Val-Asp)2-rhodamine110 by fluorescence based microplate reader analysis Induction of apoptosis in human MV4-11 cells assessed as increase in caspase 3/7 activity measured at 24 hrs in presence of Z-DEVD-R110 or (Z-Asp-Glu-Val-Asp)2-rhodamine110 by fluorescence based microplate reader analysis	[PMID: 29360358]
MV4-11	EC₅₀	2.71 μM Compound: Pic; GDC-0941	Induction of cell death in human MV4-11 cells measured at 48 hrs by fluorescence based microplate reader analysis Induction of cell death in human MV4-11 cells measured at 48 hrs by fluorescence based microplate reader analysis	[PMID: 29360358]
MV4-11	GI₅₀	3 μM Compound: GDC-0941	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
NALM-6	GI₅₀	0.15 μM Compound: 16; GDC-0941c	Growth inhibition of human NALM6 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human NALM6 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
NCI-H1650	IC₅₀	4.73 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H1650 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H1650 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
NCI-H1975	IC₅₀	0.27 μM Compound: 1, GDC-0941	Cytotoxicity against human NCI-H1975 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human NCI-H1975 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
NCI-H1975	IC₅₀	0.703 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
NCI-H1975	IC₅₀	2.42 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H1975 cells overexpressing EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells overexpressing EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
NCI-H2228	IC₅₀	1.07 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
NCI-H226	IC₅₀	2.9 μM Compound: 1, GDC-0941	Cytotoxicity against human NCI-H226 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human NCI-H226 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
NCI-H226	IC₅₀	5.91 μM Compound: GDC-0941	Antiproliferative activity against human H226 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human H226 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
NCI-H23	IC₅₀	0.936 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
NCI-H358	IC₅₀	1.33 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
NCI-H460	IC₅₀	0.87 μM Compound: 1, GDC-0941	Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
NCI-H460	IC₅₀	0.87 μM Compound: 1, GDC-0941	Cytotoxicity against human H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 25440879]
NCI-H460	IC₅₀	0.87 μM Compound: 1, GDC-0941	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 25086238]
NCI-H460	IC₅₀	1.26 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
NCI-H460	IC₅₀	2.68 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
NCI-H522	IC₅₀	2.14 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H522 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H522 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
PC-3	IC₅₀	0.2 μM Compound: GDC-0941b	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 27353887]
PC-3	IC₅₀	0.28 μM Compound: 17, GDC-0941	Antiproliferative activity against PTEN-null human PC3 cells after 96 hrs by alamar blue assay Antiproliferative activity against PTEN-null human PC3 cells after 96 hrs by alamar blue assay	[PMID: 18754654]
PC-3	EC₅₀	0.34 μM Compound: 1, GDC-0941	Antiproliferative activity against human PC3 cells after 3 to 4 days by Cell titer Glo assay Antiproliferative activity against human PC3 cells after 3 to 4 days by Cell titer Glo assay	[PMID: 21985639]
PC-3	IC₅₀	0.39 μM Compound: 2, GDC-0941	Antiproliferative activity against human PC3 cells deficient in PTEN in after 3 to 4 days Antiproliferative activity against human PC3 cells deficient in PTEN in after 3 to 4 days	[PMID: 20050669]
PC-3	IC₅₀	0.457 μM Compound: 1; GDC-0941	Antiproliferative activity against PTEN deficient human PC3 cells after 72 hrs by CCK-8 assay Antiproliferative activity against PTEN deficient human PC3 cells after 72 hrs by CCK-8 assay	[PMID: 28409639]
PC-3	IC₅₀	0.75 μM Compound: Pic; GDC-0941	Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay	[PMID: 29360358]
PC-3	IC₅₀	0.8 μM Compound: GDC-0941	Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27043268]
PC-3	IC₅₀	280 nM Compound: 1, GDC-0941	Antiproliferative activity against human PC3 cells after overnight incubation by CellTiter-Glo luminescence assay Antiproliferative activity against human PC3 cells after overnight incubation by CellTiter-Glo luminescence assay	[PMID: 21981714]
PC-3	GI₅₀	3 μM Compound: GDC-0941	Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
PF-382	GI₅₀	0.14 μM Compound: 16; GDC-0941c	Growth inhibition of human PF382 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human PF382 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
PLC-PRF-5	IC₅₀	3.07 μM Compound: Pic; GDC-0941	Antiproliferative activity against human PLC-PRF-5 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human PLC-PRF-5 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
Raji	IC₅₀	6.5 μM Compound: Pic; GDC-0941	Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
Ramos	IC₅₀	4.86 μM Compound: Pic; GDC-0941	Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
RAW	IC₅₀	298 nM Compound: 37, GDC-0941	Inhibition of human PI3Kgamma expressed in C5a-stimulated mouse RAW 264.7 cells assessed as inhibition of AKT phosphorylation by ELISA Inhibition of human PI3Kgamma expressed in C5a-stimulated mouse RAW 264.7 cells assessed as inhibition of AKT phosphorylation by ELISA	[PMID: 22548342]
Sf9	IC₅₀	0.003 μM Compound: 17, GDC-0941	Inhibition of human recombinant PI3K p110alpha expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay Inhibition of human recombinant PI3K p110alpha expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay	[PMID: 18754654]
Sf9	IC₅₀	0.003 μM Compound: 17, GDC-0941	Inhibition of human recombinant PI3K p110beta E545-K mutant expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay Inhibition of human recombinant PI3K p110beta E545-K mutant expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay	[PMID: 18754654]
Sf9	IC₅₀	0.003 μM Compound: 17, GDC-0941	Inhibition of human recombinant PI3K p110beta H1047-R mutant expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay Inhibition of human recombinant PI3K p110beta H1047-R mutant expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay	[PMID: 18754654]
Sf9	IC₅₀	0.003 μM Compound: 17, GDC-0941	Inhibition of human recombinant PI3K p110delta expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay Inhibition of human recombinant PI3K p110delta expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay	[PMID: 18754654]
Sf9	IC₅₀	0.033 μM Compound: 17, GDC-0941	Inhibition of human recombinant PI3K p110beta expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay Inhibition of human recombinant PI3K p110beta expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay	[PMID: 18754654]
Sf9	IC₅₀	17 nM Compound: 37, GDC-0941	Inhibition of GST-fused human recombinant PI3Kbeta expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presence of [gamma-33P]-ATP Inhibition of GST-fused human recombinant PI3Kbeta expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presence of [gamma-33P]-ATP	[PMID: 23540645]
Sf9	IC₅₀	42 nM Compound: 37, GDC-0941	Inhibition of human PI3Kgamma expressed in sf9 cells assessed as amount of ATP consumed by luciferase-luciferin chemiluminescence assay Inhibition of human PI3Kgamma expressed in sf9 cells assessed as amount of ATP consumed by luciferase-luciferin chemiluminescence assay	[PMID: 22548342]
SGC-7901	IC₅₀	1.8 μM Compound: 1, GDC-0941	Cytotoxicity against human SGC7901 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human SGC7901 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
SJRH30	IC₅₀	0.478 μM Compound: GDC-0941	Antiproliferative activity against human Rh30 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human Rh30 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
SJRH30	IC₅₀	0.8 μM Compound: GDC-0941	Antiproliferative activity against human Rh30 cells assessed as cell growth inhibition by SRB assay Antiproliferative activity against human Rh30 cells assessed as cell growth inhibition by SRB assay	[PMID: 32317209]
SK-BR-3	IC₅₀	0.9 μM Compound: GDC0941	Cytotoxicity against human SKBR3 cells by MTT assay Cytotoxicity against human SKBR3 cells by MTT assay	[PMID: 28006668]
SK-HEP1	IC₅₀	4.3 μM Compound: Pic; GDC-0941	Antiproliferative activity against human SK-HEP1 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human SK-HEP1 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
SK-MEL19	GI₅₀	6 μM Compound: GDC-0941	Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SK-OV-3	IC₅₀	0.864 μM Compound: 1; GDC-0941	Antiproliferative activity against human SKOV3 cells harboring PIK3CA mutant after 72 hrs by CCK-8 assay Antiproliferative activity against human SKOV3 cells harboring PIK3CA mutant after 72 hrs by CCK-8 assay	[PMID: 28409639]
SK-OV-3	GI₅₀	147.6 nM Compound: GDC-0941	Growth inhibition of human SKOV3 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay Growth inhibition of human SKOV3 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay	[PMID: 23360348]
SU-DHL-6	IC₅₀	0.03 μM Compound: Pic; GDC-0941	Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
T47D	IC₅₀	1.2 μM Compound: GDC0941	Cytotoxicity against human T47D cells by MTT assay Cytotoxicity against human T47D cells by MTT assay	[PMID: 28006668]
T47D	GI₅₀	3 μM Compound: GDC-0941	Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
U-87MG ATCC	GI₅₀	0.07 μM Compound: 61	Antiproliferative activity against human U87MG cells after 96 hrs Antiproliferative activity against human U87MG cells after 96 hrs	[PMID: 30583248]
U-87MG ATCC	IC₅₀	0.55 μM Compound: 1; GDC-0941	Antiproliferative activity against PTEN deficient human U87MG cells after 72 hrs by CCK-8 assay Antiproliferative activity against PTEN deficient human U87MG cells after 72 hrs by CCK-8 assay	[PMID: 28409639]
U-87MG ATCC	IC₅₀	0.95 μM Compound: 17, GDC-0941	Antiproliferative activity against PTEN-null human U87MG cells after 4 days by alamar blue assay Antiproliferative activity against PTEN-null human U87MG cells after 4 days by alamar blue assay	[PMID: 18754654]
U-87MG ATCC	IC₅₀	1.24 μM Compound: GDC0941	Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay	[PMID: 25911625]
U-87MG ATCC	IC₅₀	3.13 μM Compound: GDC-0941	Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
U-87MG ATCC	GI₅₀	6 μM Compound: GDC-0941	Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
U-87MG ATCC	IC₅₀	7.77 μM Compound: 1, GDC-0941	Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]

体外研究
(In Vitro)

Pictilisib (GDC-0941) 和 RP-56976 比单药治疗可将乳腺癌细胞系中的肿瘤细胞活力降低 80% 或更多。GDC-0941 可抑制 Hs578T1.2（PI3Kα 野生型）、MCF7-neo/HER2（PI3Kα 突变型）和 MX-1（PTEN 缺陷型）肿瘤模型中的 Akt 磷酸化和 Akt 信号传导的下游靶标（如 pPRAS40 和 pS6）。Pictilisib (GDC-0941) 可缩短 RP-56976 诱导的细胞凋亡前有丝分裂停滞时间^[1]。
Pictilisib (GDC-0941) 在两种 ZD1839 耐药非小细胞肺癌 (NSCLC) 细胞系 A549 和 H460 中表现出较高的抗肿瘤活性。 Pictilisib (GDC-0941) 与 U0126 联合使用可有效诱导细胞生长抑制、G0-G1 停滞和细胞凋亡。与具有野生型 PIK3CA 的 A549 细胞相比，具有 PIK3CA 激活突变的 H460 细胞对 Pictilisib (GDC-0941) 相对更敏感^[3]。
Pictilisib (GDC-0941) 可降低两种细胞系中的 PI3K 通路活性，表现为 pAK 降低。Pictilisib (GDC-0941) 可显著降低所有细胞在缺氧/缺氧暴露后在培养基中检测到的分泌性 VEGF^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Pictilisib (GDC-0941) (150 mg/kg，口服) 导致 MCF7-neo/HER2 携带动物模型中的肿瘤停滞。Pictilisib (GDC-0941) 和 RP-56976 在治疗期间导致肿瘤消退，从而增强抗肿瘤反应^[1]。
经 Pictilisib (GDC-0941) 治疗的小鼠的肿瘤显示出明显的非线性收缩，当 Pictilisib (GDC-0941) 治疗停止时，测试组小鼠的肿瘤再次生长^[2]。
Pictilisib (GDC-0941) (25 或 50 mg/kg) 抑制 eGFP-FTC133 肿瘤携带小鼠的肿瘤生长和 PI3K 和 HIF-1 通路活性^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

513.64

Formula

C₂₃H₂₇N₇O₃S₂

CAS 号

957054-30-7

性状

固体

颜色

White to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (194.69 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9469 mL	9.7344 mL	19.4689 mL
5 mM	0.3894 mL	1.9469 mL	3.8938 mL
10 mM	0.1947 mL	0.9734 mL	1.9469 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.87 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.87 mM); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (4.87 mM); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 0.5% Methyl cellulose/0.5% Tween-80 in Saline water
Solubility: 5 mg/mL (9.73 mM); Suspened solution; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.80%

选择批次：

Data Sheet (657 KB) SDS (393 KB)

COA (289 KB) HNMR (268 KB) LCMS (266 KB) 元素分析报告 (212 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Wallin JJ, et al. GDC-0941, a novel class I selective PI3K inhibitor, enhances the efficacy of RP-56976 in human breast cancer models by increasing cell death in vitro and in vivo.Clin Cancer Res. 2012 Jul 15;18(14):3901-11. Epub 2012 May 14. [Content Brief]

[2]. Wullschleger S, et al. Quantitative MRI establishes the efficacy of PI3K inhibitor (GDC-0941) multi-treatments in PTEN-deficient mice lymphoma.Anticancer Res. 2012 Feb;32(2):415-20. [Content Brief]

[3]. Zou ZQ, et al. The novel dual PI3K/mTOR inhibitor GDC-0941 synergizes with the MEK inhibitor U0126 in non-small cell lung cancer cells.Mol Med Report. 2012 Feb;5(2):503-8. [Content Brief]

[4]. Burrows N, et al. GDC-0941 inhibits metastatic characteristics of thyroid carcinomas by targeting both the phosphoinositide-3 kinase (PI3K) and hypoxia-inducible factor-1α (HIF-1α) pathways.J Clin Endocrinol Metab. 2011 Dec;96(12):E1934-43. Epub 2011 Oct [Content Brief]

[5]. Folkes AJ, et al. The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . J Med Chem. 2008 Sep 25;51(18):5522-32. [Content Brief]

[6]. Ni J, et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov. 2012 May;2(5):425-33. [Content Brief]

[7]. Cheng H, et al. A genetic mouse model of invasive endometrial cancer driven by concurrent loss of Pten and Lkb1 Is highly responsive to mTOR inhibition. Cancer Res. 2014 Jan 1;74(1):15-23. [Content Brief]

Cell Assay ^[1]	Cells are treated at EC₅₀ concentrations of Pictilisib (GDC-0941), RP-56976, or both for 4 or 24 hours and lysed in 1×Cell Extraction Buffer supplemented with protease inhibitors and Phosphatase Inhibitor Cocktails 1 and 2. Protein concentrations are determined using the Pierce BCA Protein Assay Kit. For immunoblots, equal amounts of protein are separated by electrophoresis through NuPAGE Bis-Tris 10% gradient gels, transferred onto polyvinylidene difluoride membranes using the Criterion system, and probed with monospecific primary antibodies. Specific antigen-antibody interactions are detected with IRDye 680 or IRDye 800 infrared secondary antibodies using a LI-COR imaging system. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Female nu/nu mice are inoculated subcutaneously with MCF7-neo/HER2 or MX-1 breast cancer cells. When tumors reach a mean volume of 200 to 250 mm³, animals are size-matched and distributed into groups consisting of 10 animals per group. RP-56976 formulated in 3% EtOH, 97% saline is administered intravenously once weekly. Pictilisib (GDC-0941), formulated in MCT (0.5% methylcellulose, 0.2% Tween-80) is dosed orally and daily. MAXF1162 is an HER2+/ER+/PR+ patient-derived breast cancer tumor xenograft model established by directly implanting tumors subcutaneously from patient to NMRI nu/nu mice. Tumor volume is calculated. Tumor sizes are recorded twice weekly over the course of a study. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Wallin JJ, et al. GDC-0941, a novel class I selective PI3K inhibitor, enhances the efficacy of RP-56976 in human breast cancer models by increasing cell death in vitro and in vivo.Clin Cancer Res. 2012 Jul 15;18(14):3901-11. Epub 2012 May 14. [Content Brief] [2]. Wullschleger S, et al. Quantitative MRI establishes the efficacy of PI3K inhibitor (GDC-0941) multi-treatments in PTEN-deficient mice lymphoma.Anticancer Res. 2012 Feb;32(2):415-20. [Content Brief] [3]. Zou ZQ, et al. The novel dual PI3K/mTOR inhibitor GDC-0941 synergizes with the MEK inhibitor U0126 in non-small cell lung cancer cells.Mol Med Report. 2012 Feb;5(2):503-8. [Content Brief] [4]. Burrows N, et al. GDC-0941 inhibits metastatic characteristics of thyroid carcinomas by targeting both the phosphoinositide-3 kinase (PI3K) and hypoxia-inducible factor-1α (HIF-1α) pathways.J Clin Endocrinol Metab. 2011 Dec;96(12):E1934-43. Epub 2011 Oct [Content Brief] [5]. Folkes AJ, et al. The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . J Med Chem. 2008 Sep 25;51(18):5522-32. [Content Brief] [6]. Ni J, et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov. 2012 May;2(5):425-33. [Content Brief] [7]. Cheng H, et al. A genetic mouse model of invasive endometrial cancer driven by concurrent loss of Pten and Lkb1 Is highly responsive to mTOR inhibition. Cancer Res. 2014 Jan 1;74(1):15-23. [Content Brief]

Pictilisib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9469 mL	9.7344 mL	19.4689 mL	48.6722 mL
	5 mM	0.3894 mL	1.9469 mL	3.8938 mL	9.7344 mL
	10 mM	0.1947 mL	0.9734 mL	1.9469 mL	4.8672 mL
	15 mM	0.1298 mL	0.6490 mL	1.2979 mL	3.2448 mL
	20 mM	0.0973 mL	0.4867 mL	0.9734 mL	2.4336 mL
	25 mM	0.0779 mL	0.3894 mL	0.7788 mL	1.9469 mL
	30 mM	0.0649 mL	0.3245 mL	0.6490 mL	1.6224 mL
	40 mM	0.0487 mL	0.2434 mL	0.4867 mL	1.2168 mL
	50 mM	0.0389 mL	0.1947 mL	0.3894 mL	0.9734 mL
	60 mM	0.0324 mL	0.1622 mL	0.3245 mL	0.8112 mL
	80 mM	0.0243 mL	0.1217 mL	0.2434 mL	0.6084 mL
	100 mM	0.0195 mL	0.0973 mL	0.1947 mL	0.4867 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pictilisib957054-30-7GDC-0941GDC0941GDC 0941PI3KAutophagyApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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Pictilisib (Synonyms: GDC-0941)

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Pictilisib (Synonyms: GDC-0941)

Customer Review

Other Forms of Pictilisib:

Pictilisib 相关抗体

MCE 顾客使用本产品发表的 50 篇科研文献

Pictilisib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 PI3K 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Pictilisib 相关抗体:

摩尔计算器

稀释计算器

Pictilisib 相关分类

完整储备液配制表

Keywords:

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