Idelalisib (Synonyms: 艾代拉里斯; CAL-101; GS-1101)

目录号: HY-13026 纯度: 99.58%: FAQs
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摩尔计算器

Idelalisib (CAL-101; GS-1101) 是一种口服有效的高选择性 p110δ 抑制剂，IC₅₀ 为 2.5 nM，比 p110δ 和其他 PI3K class I 酶的选择性高 40 到 300 倍。

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Idelalisib Chemical Structure

CAS No. : 870281-82-6

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥347	In-stock
1 mg	￥190	In-stock
5 mg	￥380	In-stock
10 mg	￥550	In-stock
25 mg	￥990	In-stock
50 mg	￥1300	In-stock
100 mg	￥1975	In-stock
200 mg	￥2975	In-stock
500 mg	￥4938	In-stock
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5 g		询价

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Customer Review

Other Forms of Idelalisib:

Idelalisib-d₅ In-stock

MCE 顾客使用本产品发表的 44 篇科研文献

Proliferation Assay

: Idelalisib 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.

: Idelalisib 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.

: Idelalisib purchased from MCE. Usage Cited in: Br J Haematol. 2015 Jul;170(1):134-8. [Abstract]; Treatment of CXCR4^WT and CXCR4^S338X BCWM.1 and MWCL-1 cells with PCI-32765 or Idelalisib induced caspase-3 and PARP cleavage at 6 h. Caspase-3 and PAPR cleavage following PCI-32765 (IB), Idelalisib (ID), ABT-199 (ABT), in the presence of absence of CXCL12 (SDF) and AMD3100 (AMD).

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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

Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC₅₀ of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.

IC₅₀ & Target^[1]

p110δ

2.5 nM (IC₅₀)

p110γ

89 nM (IC₅₀)

p110β

565 nM (IC₅₀)

p110α

820 nM (IC₅₀)

hVps34

978 nM (IC₅₀)

DNA-PK

6729 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A498	GI₅₀	1.1 μM Compound: Idelalisib	Antiproliferative activity against human A498 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human A498 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
A549	IC₅₀	0.33 μM Compound: CAL-101	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	10.1039/C5MD00364D
B-cell	IC₅₀	0.0061 μM Compound: 74, GS-1101, CAL-101	Inhibition of PI3Kdelta in B-cells by proliferation assay Inhibition of PI3Kdelta in B-cells by proliferation assay	[PMID: 22924688]
Bel-7402	IC₅₀	66.23 μM Compound: CAL-101	Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35191698]
CAKI-1	GI₅₀	20.5 μM Compound: Idelalisib	Antiproliferative activity against human Caki1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human Caki1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
CCRF-CEM	GI₅₀	22.3 μM Compound: Idelalisib	Antiproliferative activity against human CCRF-CEM cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human CCRF-CEM cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
DOHH-2	IC₅₀	0.86 μM Compound: Idelalisib	Cytotoxicity against human DOHH-2 cells expressing BTK and PI3kdelta assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Cytotoxicity against human DOHH-2 cells expressing BTK and PI3kdelta assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 35247756]
HCC 2998	GI₅₀	38.5 μM Compound: Idelalisib	Antiproliferative activity against human HCC2998 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HCC2998 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
HCT-116	IC₅₀	> 10 μM Compound: Idelalisib	Antiproliferative activity against human HCT116 cells by MTT assay Antiproliferative activity against human HCT116 cells by MTT assay	[PMID: 31434616]
HCT-116	IC₅₀	2.96 μM Compound: 1	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
HEK293	IC₅₀	> 20 μM Compound: Idelalisib	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability by MTS assay Cytotoxicity against human HEK293 cells assessed as reduction in cell viability by MTS assay	[PMID: 32784091]
HeLa	IC₅₀	0.15 μM Compound: CAL-101	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	10.1039/C5MD00364D
Hep 3B2	IC₅₀	77.55 μM Compound: CAL-101	Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35191698]
HepG2	IC₅₀	0.92 μM Compound: CAL-101	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	10.1039/C5MD00364D
HepG2	IC₅₀	89.5 μM Compound: CAL-101	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35191698]
HOP-62	GI₅₀	> 100 μM Compound: Idelalisib	Antiproliferative activity against human HOP62 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HOP62 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
HOP-92	GI₅₀	14.1 μM Compound: Idelalisib	Antiproliferative activity against human HOP92 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HOP92 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
Hs-578T	GI₅₀	6 μM Compound: Idelalisib	Antiproliferative activity against human Hs578T cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human Hs578T cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
HT	IC₅₀	> 10 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human HT cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human HT cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
HUVEC	IC₅₀	38.22 μM Compound: 1	Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
IGROV-1	GI₅₀	4.8 μM Compound: Idelalisib	Antiproliferative activity against human IGROV1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human IGROV1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
JeKo-1	IC₅₀	0.12 μM Compound: Idelalisib	Antiproliferative activity against human JeKo-1 assessed as reduction in cell growth by MTS assay Antiproliferative activity against human JeKo-1 assessed as reduction in cell growth by MTS assay	[PMID: 32784091]
Jurkat	IC₅₀	7.9 μM Compound: Idelalisib	Antiproliferative activity against human Jurkat cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human Jurkat cells after 3 days by CellTiter-Glo assay	[PMID: 27774127]
KARPAS-422	GI₅₀	0.68 μM Compound: CAL-101	Growth inhibition of human KARPAS422 cells by CCK8 assay Growth inhibition of human KARPAS422 cells by CCK8 assay	[PMID: 28835805]
KARPAS-422	IC₅₀	8.1 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human KARPAS422 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human KARPAS422 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
KM12	IC₅₀	0.96 μM Compound: 1	Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
KM12	GI₅₀	1.2 μM Compound: Idelalisib	Antiproliferative activity against human KM12 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human KM12 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
L02	IC₅₀	> 20 μM Compound: Idelalisib	Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTS assay Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTS assay	[PMID: 32784091]
LOUCY	IC₅₀	8.4 μM Compound: Idelalisib	Antiproliferative activity against human Loucy cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human Loucy cells after 3 days by CellTiter-Glo assay	[PMID: 27774127]
LOX IMVI	GI₅₀	33.5 μM Compound: Idelalisib	Antiproliferative activity against human LOXIMVI cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human LOXIMVI cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
M14	GI₅₀	37.8 μM Compound: Idelalisib	Antiproliferative activity against human M14 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human M14 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
MCF7	IC₅₀	> 10 μM Compound: Idelalisib	Antiproliferative activity against human MCF7 cells by MTT assay Antiproliferative activity against human MCF7 cells by MTT assay	[PMID: 31434616]
MCF7	IC₅₀	0.78 μM Compound: CAL-101	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	10.1039/C5MD00364D
MDA-MB-231	GI₅₀	42.3 μM Compound: Idelalisib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
MOLM-13	GI₅₀	1.7 μM Compound: 1; CAL-101	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	IC₅₀	3.6 μM Compound: Idelalisib	Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo assay	[PMID: 27774127]
MOLM-14	GI₅₀	6.4 μM Compound: 1; CAL-101	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	> 10 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human MOLT4 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human MOLT4 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
MOLT-4	IC₅₀	10.6 μM Compound: Idelalisib	Antiproliferative activity against human MOLT4 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human MOLT4 cells after 3 days by CellTiter-Glo assay	[PMID: 27774127]
MRC5	IC₅₀	> 100 μM Compound: 1; 6c	Cytotoxicity against human MRC5 cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay	[PMID: 34332211]
MV4-11	GI₅₀	> 10 μM Compound: 1; CAL-101	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	6.3 μM Compound: Idelalisib	Antiproliferative activity against human MV4-11 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells after 3 days by CellTiter-Glo assay	[PMID: 27774127]
NALM-6	GI₅₀	> 10 μM Compound: 1; CAL-101	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]
NAMALVA	IC₅₀	> 10 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human NAMALWA cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human NAMALWA cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
Neutrophil	IC₅₀	0.07 μM Compound: Idelalisib	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation by measuring superoxide oxide dismutase inhibitable reduction of ferricytochrome c incubated for 5 mins Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation by measuring superoxide oxide dismutase inhibitable reduction of ferricytochrome c incubated for 5 mins	[PMID: 28648460]
Neutrophil	IC₅₀	0.07 μM Compound: Idelalisib	Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of superoxide generation preincubated for 5 mins followed by cytochalasin B and FMLP stimulation for 3 mins and 10 mins respectively by ferricytochrome c reduction b Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of superoxide generation preincubated for 5 mins followed by cytochalasin B and FMLP stimulation for 3 mins and 10 mins respectively by ferricytochrome c reduction b	[PMID: 27142697]
Neutrophil	IC₅₀	0.1 μM Compound: CAL-101	Antiinflammatory activity in human neutrophils assessed as inhibition of FMLP/cytochalasin B-induced superoxide anion generation by measuring superoxide dismutase-inhibitable reduction of ferricytochrome c preincubated for 5 mins followed by FMLP/cytochal Antiinflammatory activity in human neutrophils assessed as inhibition of FMLP/cytochalasin B-induced superoxide anion generation by measuring superoxide dismutase-inhibitable reduction of ferricytochrome c preincubated for 5 mins followed by FMLP/cytochal	[PMID: 27525452]
Neutrophil	IC₅₀	0.3 μM Compound: Idelalisib	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release incubated for 5 mins in presence of MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release incubated for 5 mins in presence of MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide	[PMID: 28648460]
Neutrophil	IC₅₀	0.3 μM Compound: CAL-101	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as elastase substrate preincubated for 5 mins followed by fMLP/CB-induction Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as elastase substrate preincubated for 5 mins followed by fMLP/CB-induction	[PMID: 27525452]
Neutrophil	IC₅₀	0.3 μM Compound: Idelalisib	Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of elastase release preincubated for 5 mins followed by FMLP/CB stimulation for 10 mins using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of elastase release preincubated for 5 mins followed by FMLP/CB stimulation for 10 mins using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate	[PMID: 27142697]
OCI-Ly10	IC₅₀	> 10 μM Compound: Idelalisib	Antiproliferative activity against human OCILY10 assessed as reduction in cell growth by MTS assay Antiproliferative activity against human OCILY10 assessed as reduction in cell growth by MTS assay	[PMID: 32784091]
OCI-Ly10	IC₅₀	31.9 nM Compound: 1; CAL-101	Anticancer activity against human OCILY10 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay Anticancer activity against human OCILY10 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay	[PMID: 33297683]
OCI-Ly3	IC₅₀	5.2 μM Compound: Idelalisib	Antiproliferative activity against human OCILY3 assessed as reduction in cell growth by MTS assay Antiproliferative activity against human OCILY3 assessed as reduction in cell growth by MTS assay	[PMID: 32784091]
OVCAR-3	GI₅₀	17.7 μM Compound: Idelalisib	Antiproliferative activity against human OVCAR3 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human OVCAR3 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
PF-382	GI₅₀	> 10 μM Compound: 1; CAL-101	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]
Pfeiffer	GI₅₀	0.74 μM Compound: CAL-101	Growth inhibition of human Pfeiffer cells by CCK8 assay Growth inhibition of human Pfeiffer cells by CCK8 assay	[PMID: 28835805]
Pfeiffer	IC₅₀	6.8 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human Pfeiffer cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human Pfeiffer cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
Raji	IC₅₀	> 10 μM Compound: Idelalisib	Antiproliferative activity against human Raji cells by MTT assay Antiproliferative activity against human Raji cells by MTT assay	[PMID: 31434616]
Raji	IC₅₀	9.95 nM Compound: Idelalisib	Antiproliferative activity against human Raji cells after 72 hrs by MTT assay Antiproliferative activity against human Raji cells after 72 hrs by MTT assay	[PMID: 28325601]
Raji	IC₅₀	9.95 μM Compound: 1; CAL-101	Antiproliferative activity against human Raji cells after 72 hrs by MTT assay Antiproliferative activity against human Raji cells after 72 hrs by MTT assay	[PMID: 29534936]
Ramos	IC₅₀	> 10 nM Compound: Idelalisib	Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay	[PMID: 28325601]
Ramos	IC₅₀	> 10 μM Compound: 1; CAL-101	Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay	[PMID: 29534936]
Ramos	IC₅₀	> 10 μM Compound: Idelalisib	Antiproliferative activity against human Ramos cells by MTT assay Antiproliferative activity against human Ramos cells by MTT assay	[PMID: 31434616]
Ramos	IC₅₀	0.004 μM Compound: 1; CAL-101, GS-1101	Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in antihuman IgM-stimulated AKT phosphorylation at Ser473 residue preincubated for 60 mins followed by antihuman IgM stimulation and measured after 15 mins Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in antihuman IgM-stimulated AKT phosphorylation at Ser473 residue preincubated for 60 mins followed by antihuman IgM stimulation and measured after 15 mins	[PMID: 31033293]
RAW264.7	IC₅₀	0.337 μM Compound: 1; CAL-101, GS-1101	Inhibition of PI3Kgamma in rat RAW264.7 cells assessed as reduction in C5a-stimulated AKT phosphorylation at Ser473 residue preincubated for 30 mins followed by C5a-stimulation and measured after 5 mins Inhibition of PI3Kgamma in rat RAW264.7 cells assessed as reduction in C5a-stimulated AKT phosphorylation at Ser473 residue preincubated for 30 mins followed by C5a-stimulation and measured after 5 mins	[PMID: 31033293]
RPMI-8226	IC₅₀	5.49 μM Compound: 1; CAL-101	Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay	[PMID: 29534936]
RXF 393	GI₅₀	1.4 μM Compound: Idelalisib	Antiproliferative activity against human RXF393 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human RXF393 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
Sf21	IC₅₀	0.002 μM Compound: 1; CAL-101, GS-1101	Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence po Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence po	[PMID: 31033293]
Sf21	IC₅₀	0.293 μM Compound: 1; CAL-101, GS-1101	Inhibition of N-terminal His6-tagged recombinant full length human p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence pol Inhibition of N-terminal His6-tagged recombinant full length human p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence pol	[PMID: 31033293]
Sf21	IC₅₀	154 nM Compound: 1	Inhibition of His6-tagged recombinant full length human N-terminal PI3Kbeta expressed in baculovirus infected Sf21 cells using lipid substrate incubated for 2 hrs by ADP-Glo assay Inhibition of His6-tagged recombinant full length human N-terminal PI3Kbeta expressed in baculovirus infected Sf21 cells using lipid substrate incubated for 2 hrs by ADP-Glo assay	[PMID: 30878826]
SNB-75	GI₅₀	1.2 μM Compound: Idelalisib	Antiproliferative activity against human SNB75 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human SNB75 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
SUD4	IC₅₀	1.6 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human SU-DHL4 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human SU-DHL4 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
SU-DHL-1	IC₅₀	> 10 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human SU-DHL1 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human SU-DHL1 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
SU-DHL10	IC₅₀	> 10 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human SU-DHL10 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human SU-DHL10 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
SU-DHL-6	GI₅₀	0.02 μM Compound: 1	Antiproliferative activity against human SU-DHL6 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human SU-DHL6 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30996859]
SU-DHL-6	IC₅₀	0.033 μM Compound: Idelalisib	Antiproliferative activity against human SUDHL6 cells by MTT assay Antiproliferative activity against human SUDHL6 cells by MTT assay	[PMID: 31434616]
SU-DHL-6	GI₅₀	0.042 μM Compound: CAL-101; 1	Growth inhibition of human SU-DHL6 cells by CellTiter-Glo assay Growth inhibition of human SU-DHL6 cells by CellTiter-Glo assay	[PMID: 29601991]
SU-DHL-6	IC₅₀	0.053 μM Compound: 1	Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
SU-DHL-6	IC₅₀	0.12 μM Compound: Idelalisib	Antiproliferative activity against human SU-DHL-6 assessed as reduction in cell growth by MTS assay Antiproliferative activity against human SU-DHL-6 assessed as reduction in cell growth by MTS assay	[PMID: 32784091]
SU-DHL-6	IC₅₀	0.65 μM Compound: 1; CAL-101	Antiproliferative activity against human SUDHL6 cells after 72 hrs by CCK8 assay Antiproliferative activity against human SUDHL6 cells after 72 hrs by CCK8 assay	[PMID: 29534936]
SU-DHL-6	IC₅₀	117.6 nM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human SUDHL6 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human SUDHL6 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
SU-DHL-6	GI₅₀	124 nM Compound: 1	Growth inhibition of human SU-DHL6 cells incubated for 72 hrs by CellTiter-Glo assay Growth inhibition of human SU-DHL6 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 30878826]
SU-DHL-6	IC₅₀	22.5 nM Compound: 1; CAL-101	Anticancer activity against human SUDHL-6 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay Anticancer activity against human SUDHL-6 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay	[PMID: 33297683]
SU-DHL-6	GI₅₀	34 nM Compound: Idelalisib	Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32078865]
T47D	IC₅₀	0.51 μM Compound: 1	Antiproliferative activity against human T47D cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human T47D cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
T47D	GI₅₀	5.2 μM Compound: Idelalisib	Antiproliferative activity against human T47D cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human T47D cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
TMD8	IC₅₀	7.3 nM Compound: 1; CAL-101	Anticancer activity against human TMD8 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay Anticancer activity against human TMD8 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay	[PMID: 33297683]
U-251	GI₅₀	53.2 μM Compound: Idelalisib	Antiproliferative activity against human U251 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human U251 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
Vero	IC₅₀	> 20 μM Compound: Idelalisib	Cytotoxicity against monkey Vero cells assessed as reduction in cell viability by MTS assay Cytotoxicity against monkey Vero cells assessed as reduction in cell viability by MTS assay	[PMID: 32784091]

体外研究
(In Vitro)

Idelalisib (CAL-101; GS-1101) 是一种高选择性、强效的 p110δ 抑制剂 (EC₅₀=8 nM)。对相关激酶 C2β、hVPS34、DNA-PK 和 mTOR 具有更高的选择性（400 至 4000 倍），而对 402 种不同的激酶在 10 μM 时没有观察到活性。CAL-101 在 10 μM 时仅将 PDGF 诱导的 pAkt 降低 25%。Idelalisib (CAL-101) 抑制 LPA 诱导的 pAkt，EC₅₀ 为 1.9 μM。 Idelalisib (CAL-101) 阻断 Fc-RI p110δ 介导的 CD63 表达，EC₅₀ 为 8 nM；抑制 p110γ 的甲酰-甲硫氨酰-亮氨酰-苯丙氨酸活化，EC₅₀ 为 3 μM。因此，在基于细胞的测定中，CAL-101 对 p110δ 的选择性是其他 I 类 PI3K 亚型的 240 至 2500 倍^[1]。
CAL-101 Idelalisib (CAL-101) 诱导的慢性淋巴细胞白血病 (CLL) 细胞凋亡与单独使用载体治疗相比显著 (P<0.001)。 Idelalisib (CAL-101) 在 CLL 细胞中诱导选择性细胞毒性，与 IgVH 突变状态或间期细胞遗传学无关^[2]。

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

体内研究
(In Vivo)

在 p110δ^D910A/D910A 小鼠和 Idelalisib (CAL-101) (40 mg/kg，iv) 治疗后小鼠的脑匀浆中，CD11b⁺Ly6G⁺ 中性粒细胞均显著减少^[3]。

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

Clinical Trial

分子量

415.42

Formula

C₂₂H₁₈FN₇O

CAS 号

870281-82-6

性状

固体

颜色

White to off-white

中文名称

艾代拉里斯；艾代拉利司；艾拉利司

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	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 59.7 mg/mL (143.71 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4072 mL	12.0360 mL	24.0720 mL
5 mM	0.4814 mL	2.4072 mL	4.8144 mL
10 mM	0.2407 mL	1.2036 mL	2.4072 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

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 (6.02 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 (6.02 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 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 (6.02 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，此方案实验周期在半个月以上的动物实验酌情使用。
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。

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: 99.78%

选择批次：

Data Sheet (654 KB) SDS (393 KB)

COA (201 KB) LCMS (120 KB) 元素分析报告 (218 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Lannutti BJ, et al. CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood, 2011, 117(2), 591-594. [Content Brief]

[2]. Herman SE, et al. Phosphatidylinositol 3-kinase-δ inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals. Blood, 2010, 116(12), 2078-2088. [Content Brief]

[3]. Low PC, et al. PI3Kδ inhibition reduces TNF secretion and neuroinflammation in a mouse cerebral stroke model. Nat Commun. 2014 Mar 14;5:3450. [Content Brief]

[4]. Cooney J, et al. Synergistic targeting of the regulatory and catalytic subunits of PI3Kδ in mature B cell malignancies. Clin Cancer Res. 2018 Mar 1;24(5):1103-1113. [Content Brief]

Cell Assay ^[2]	MTT assays are performed to determine cytotoxicity. Briefly, 1×10⁵ cells (CLL B cells or healthy volunteer T cells or NK cells) are incubated for 48 hours with different concentrations of Idelalisib (CAL-101) (0.1 μM, 1 μM, 5 μM, 10 μM), 25 μM LY294002, or vehicle control. MTT reagent is then added. DMSO is added, and absorbance is measured by spectrophotometry at 540 nm in a Labsystems plate reader. Cell viability is also measured at various time points with the use of annexin/PI flow cytometry. Data are analyzed with Expo-ADC32 software package. At least 10,000 cells are counted for each sample. Results are expressed as the percentage of total positive cells over untreated control. Experiments examining caspase-dependent apoptosis included the addition of 100 μM Z-VAD. Experiments examining survival signals include the addition of 1 μg/mL CD40L, 800 U/mL IL-4, 50 ng/mL BAFF, 20 ng/mL TNF-α, or coculturing on fibronectin or stromal (HS-5 cell line) coated plates. Stromal coculture is done by plating a 75-cm2 flask (80%-100% confluent) per 6-well plate 24 hours before the addition of CLL cells^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Mice^[3] For Idelalisib (CAL-101) treatment, wild-type C57BL/6 mice are administered either 40 mg/kg Idelalisib (CAL-101) or vehicle DMSO, by 25 μL infusion into the femoral vein, 15 min before I/R (pre-treatment), or 3 and 6 h after initiation of reperfusion (post-treatment). Controls and animals treated with Idelalisib (CAL-101) underwent cerebral blood flow (CBF) measurements using a laser Doppler perfusion monitor. The CBF measurements obtained immediately before and after MCAO and again at 3 h after reperfusion showed an ~90-95% reduction in the blood flow to the MCAO infarct region, which does not differ between groups. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Lannutti BJ, et al. CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood, 2011, 117(2), 591-594. [Content Brief] [2]. Herman SE, et al. Phosphatidylinositol 3-kinase-δ inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals. Blood, 2010, 116(12), 2078-2088. [Content Brief] [3]. Low PC, et al. PI3Kδ inhibition reduces TNF secretion and neuroinflammation in a mouse cerebral stroke model. Nat Commun. 2014 Mar 14;5:3450. [Content Brief] [4]. Cooney J, et al. Synergistic targeting of the regulatory and catalytic subunits of PI3Kδ in mature B cell malignancies. Clin Cancer Res. 2018 Mar 1;24(5):1103-1113. [Content Brief]

Idelalisib 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	2.4072 mL	12.0360 mL	24.0720 mL	60.1801 mL
	5 mM	0.4814 mL	2.4072 mL	4.8144 mL	12.0360 mL
	10 mM	0.2407 mL	1.2036 mL	2.4072 mL	6.0180 mL
	15 mM	0.1605 mL	0.8024 mL	1.6048 mL	4.0120 mL
	20 mM	0.1204 mL	0.6018 mL	1.2036 mL	3.0090 mL
	25 mM	0.0963 mL	0.4814 mL	0.9629 mL	2.4072 mL
	30 mM	0.0802 mL	0.4012 mL	0.8024 mL	2.0060 mL
	40 mM	0.0602 mL	0.3009 mL	0.6018 mL	1.5045 mL
	50 mM	0.0481 mL	0.2407 mL	0.4814 mL	1.2036 mL
	60 mM	0.0401 mL	0.2006 mL	0.4012 mL	1.0030 mL
	80 mM	0.0301 mL	0.1505 mL	0.3009 mL	0.7523 mL
	100 mM	0.0241 mL	0.1204 mL	0.2407 mL	0.6018 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:

Idelalisib870281-82-6CAL-101 GS-1101艾代拉里斯艾代拉利司艾拉利司CAL101CAL 101GS1101GS 1101GS-1101PI3KAutophagyPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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Idelalisib (Synonyms: 艾代拉里斯; CAL-101; GS-1101)

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Idelalisib (Synonyms: 艾代拉里斯; CAL-101; GS-1101)

Customer Review

Other Forms of Idelalisib:

Idelalisib 相关抗体

MCE 顾客使用本产品发表的 44 篇科研文献

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