Palbociclib (Synonyms: 帕博西尼; PD 0332991)

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摩尔计算器

Palbociclib (PD 0332991) 是一种具有口服活性的 CDK4 和 CDK6 选择性抑制剂，IC₅₀ 值分别为 11 nM 和16 nM。Palbociclib 对癌细胞具有抗增殖活性，并诱导其细胞周期阻滞，可用于 HR 阳性和 HER2 阴性乳腺癌，以及肝细胞癌的相关研究。

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Palbociclib Chemical Structure

CAS No. : 571190-30-2

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Customer Review

Other Forms of Palbociclib:

MCE 顾客使用本产品发表的 157 篇科研文献

IHC

: Palbociclib purchased from MCE. Usage Cited in: Life Sciences. 2023 Apr 1, 121652.; Palbociclib (1 µM; 48 h) decreases the expression of PPARγ in SVFs.

: Palbociclib purchased from MCE. Usage Cited in: EBioMedicine. 2019 May;43:225-237. [Abstract]; Representative images of immunohistochemical staining for proteins as indicated in A2780 xenografted tumors (n=6 per treatment group) treated with AZD2281 and Palbociclib either as single-agents or in combination for 4 days.

: Palbociclib purchased from MCE. Usage Cited in: Nat Commun. 2018 Oct 9;9(1):4180. [Abstract]; MCF7, MCF7-LEM4, and MCF7-TAMR cells are treated with 5% DCC-FBS (vehicle), 4-OHT (1 μM), PD0332991 (PD) (0.2 μM), or a combination of 4-OHT and PD0332991. Immunoblots of lysates from cells are tested.

: Palbociclib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Sep 20;37(1):233. [Abstract]; Western blot of the nine cell cycle-related proteins in C666-1 cells treated with different concentrations of GEM (0.1, 1, and 10 μM) and PAL (0.1, 1, and 5 μM) after 48 h.

: Palbociclib purchased from MCE. Usage Cited in: Eur J Cancer. 2018 Oct;102:10-22. [Abstract]; Head-to-head comparison of the effect of Palbociclib and Ribociclib on DNA damage response (DDR) signalling in liver cancer cells.

: Palbociclib purchased from MCE. Usage Cited in: Nature. 2017 Jun 15;546(7658):426-430. [Abstract]; In vitro kinase reactions using immunoprecipitated endogenous CDK6 and recombinant PFKP or PKM2 with or without Palbociclib (PALBO). ³²P-PFKP and ³²P-PKM2 denote phosphorylated proteins, IB, immunoblotting.

: Palbociclib purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]; Effects of Palbociclib on CDK4/6-Rb pathway. HCC cells are treated with different doses of Palbociclib for 24 h, and then, the cells are subjected to western blot analysis.

: Palbociclib purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]; Effects of CDK4/6 inhibitors on AMPK phosphorylation and apoptosis-related signals. After 24 h of drug treatment, the cells are subjected to western blot analysis. AMPK phosphorylation level is quantified by the ratio of band intensities of phospho-AMPKα vs. AMPKα.

: Palbociclib purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]; Inhibition of AMPK reverses Palbociclib-induced autophagy and apoptosis. Hep3B cells are incubated with AMPK inhibitor (Compound C, 2.5 μM) for 4 h and then treated with Palbociclib for 24 h. Apoptotic cells are determined by flow cytometry.

: Palbociclib purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2017 Nov 20;1865(2):354-363. [Abstract]; LAPC-4 cells are grown in charcoal-stripped serum medium (CSS) for 24 hours and then stimulated by R1881 alone or with different doses of Palbociclib (PD). Palbociclib is added 30 min before androgen treatment. Cellular expression of all proteins is detected by immunoblotting analysis. β-actin is included as a control for protein loading.

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

生物活性
纯度 & 产品资料
参考文献

生物活性

Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC₅₀ values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma^[1]^[3]^[4].

IC₅₀ & Target^[1]

Cdk4/cyclin D3

9 nM (IC₅₀)

Cdk4/cyclin D1

11 nM (IC₅₀)

Cdk6/cyclin D2

16 nM (IC₅₀)

DYRK1A

2000 nM (IC₅₀)

MAPK

8000 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A2780	GI₅₀	0.032 μM Compound: Palbociclib	Growth inhibition of human A2780 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human A2780 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
A549	IC₅₀	> 10 μM Compound: Palbociclib	Antiproliferative activity against human A549 cells assessed as growth inhibition by CCK-8 assay Antiproliferative activity against human A549 cells assessed as growth inhibition by CCK-8 assay	[PMID: 36130661]
A549	EC₅₀	0.4 μM Compound: Palbociclib	Growth inhibition of human A549 cells measured after 72 hrs by propidium iodide staining based fluorescence assay Growth inhibition of human A549 cells measured after 72 hrs by propidium iodide staining based fluorescence assay	[PMID: 30665142]
A549	IC₅₀	1.32 μM Compound: V	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: 30572179]
A549	IC₅₀	8.07 μM Compound: Palbociclib	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: 37011445]
A549	IC₅₀	9.4 μM Compound: Palbociclib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34624191]
BPH-1	GI₅₀	7.442 μM Compound: Palbociclib	Growth inhibition of nontransformed human BPH1 cells after 72 hrs by resazurin or MTT assay Growth inhibition of nontransformed human BPH1 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
Calu-1	EC₅₀	33 μM Compound: Palbociclib	Growth inhibition of human Calu1 cells measured after 72 hrs by propidium iodide staining based fluorescence assay Growth inhibition of human Calu1 cells measured after 72 hrs by propidium iodide staining based fluorescence assay	[PMID: 30665142]
COLO 205	IC₅₀	0.036 μM Compound: Palbociclib	Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis	[PMID: 24641103]
COLO 205	IC₅₀	300.6 nM Compound: Palbociclib	Antiproliferative activity against human COLO 205 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay Antiproliferative activity against human COLO 205 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay	[PMID: 32200202]
CWR22R	GI₅₀	0.435 μM Compound: Palbociclib	Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
DU-145	GI₅₀	5.792 μM Compound: Palbociclib	Growth inhibition of human DU145 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human DU145 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
DU-145	IC₅₀	7.5 μM Compound: 31, PD-0332991	Cytotoxicity against human DU145 cells after 96 hrs by Cell-Titer Blue assay Cytotoxicity against human DU145 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 24417566]
HCC38	EC₅₀	1.4 μM Compound: 51	Anticancer activity against human HCC38 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis Anticancer activity against human HCC38 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis	[PMID: 33650861]
HCT-116	IC₅₀	> 10 μM Compound: Palbociclib	Antiproliferative activity against human HCT-116 cells assessed as growth inhibition by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as growth inhibition by CCK-8 assay	[PMID: 36130661]
HCT-116	IC₅₀	7.11 μM Compound: 1	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 33197548]
HCT-116	IC₅₀	8.9 μM Compound: V	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
HEK293	GI₅₀	9.608 μM Compound: Palbociclib	Antiproliferative activity against human HEK293 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human HEK293 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
HeLa	IC₅₀	> 10 μM Compound: Palbociclib	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34624191]
HeLa	IC₅₀	13.3 μM Compound: 1	Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 33197548]
HepG2	IC₅₀	> 10 μM Compound: Palbociclib	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34624191]
HepG2	IC₅₀	9.92 μM Compound: Palbociclib	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37011445]
HL-60	GI₅₀	29.17 μM Compound: Palbociclib	Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay	[PMID: 34958208]
HL-60	GI₅₀	3.498 μM Compound: Palbociclib	Antiproliferative activity against human HL-60 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
HT-29	IC₅₀	3.56 μM Compound: 1	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 33197548]
HT-29	IC₅₀	9.3 μM Compound: Palbociclib	Antiproliferative activity against human HT-29 cells assessed as growth inhibition by CCK-8 assay Antiproliferative activity against human HT-29 cells assessed as growth inhibition by CCK-8 assay	[PMID: 36130661]
JeKo-1	GI₅₀	30 μM Compound: Palbociclib	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]
Jurkat	GI₅₀	> 100 μM Compound: Palbociclib	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
K562	IC₅₀	> 10 μM Compound: Palbociclib	Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34624191]
K562	IC₅₀	2 μM Compound: 31, PD-0332991	Cytotoxicity against human K562 cells after 96 hrs by Cell-Titer Blue assay Cytotoxicity against human K562 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 24417566]
K562	GI₅₀	2.455 μM Compound: Palbociclib	Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
L02	GI₅₀	> 100 μM Compound: Palbociclib	Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
LNCaP C4-2B	GI₅₀	4.15 μM Compound: Palbociclib	Growth inhibition of human C4-2B cells after 72 hrs by resazurin or MTT assay Growth inhibition of human C4-2B cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
MCF-10A	GI₅₀	19.07 μM Compound: Palbociclib	Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36350721]
MCF7	IC₅₀	> 10 μM Compound: Palbociclib	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34624191]
MCF7	GI₅₀	> 100 μM Compound: Palbociclib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
MCF7	IC₅₀	0.34 μM Compound: PD0332991	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33857728]
MCF7	GI₅₀	0.557 μM Compound: Palbociclib	Growth inhibition of human MCF7 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human MCF7 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
MCF7	IC₅₀	0.78 μM Compound: Palbociclib	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: 37011445]
MCF7	IC₅₀	240 nM Compound: 1	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 27448913]
MCF7	GI₅₀	3.938 μM Compound: Palbociclib	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36350721]
MCF7	IC₅₀	4.09 μM Compound: V	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
MCF7	IC₅₀	5.81 μM Compound: Palbociclib	Antiproliferative activity against palbociclib-resistant human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against palbociclib-resistant human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37011445]
MDA-MB-231	GI₅₀	> 100 μM Compound: Palbociclib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
MDA-MB-231	EC₅₀	0.3 μM Compound: 51	Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis	[PMID: 33650861]
MDA-MB-231	IC₅₀	14.6 μM Compound: Paldociclib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs	[PMID: 33139111]
MDA-MB-231	IC₅₀	3.5 μM Compound: V	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: 30572179]
MDA-MB-231	GI₅₀	30 μM Compound: Palbociclib	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	4.72 μM Compound: PD0332991	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33857728]
MDA-MB-231	IC₅₀	5.62 μM Compound: Palbociclib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37011445]
MDA-MB-231	IC₅₀	580 nM Compound: 1	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 27448913]
MDA-MB-231	IC₅₀	6.21 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 33197548]
MDA-MB-435	IC₅₀	0.16 μM Compound: 43(table 3)	Inhibitory concentration was measured by the incorporation of [14C]-thymidine in (human breast carcinoma) MDA-MB-435 cell line Inhibitory concentration was measured by the incorporation of [14C]-thymidine in (human breast carcinoma) MDA-MB-435 cell line	[PMID: 15801831]
MDA-MB-435	IC₅₀	160 nM Compound: PD-0332991	Antiproliferative activity against Rb-positive human MDA-MB-435 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis Antiproliferative activity against Rb-positive human MDA-MB-435 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis	[PMID: 26115571]
MDA-MB-436	EC₅₀	5 μM Compound: 51	Anticancer activity against human MDA-MB-436 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis Anticancer activity against human MDA-MB-436 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis	[PMID: 33650861]
MDA-MB-453	GI₅₀	0.326 μM Compound: Palbociclib	Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay	[PMID: 28156111]
MDA-MB-453	IC₅₀	137 nM Compound: 1	Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 27448913]
MDA-MB-453	IC₅₀	6.93 μM Compound: PD0332991	Antiproliferative activity against human MDA-MB-453 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-453 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33857728]
MDA-MB-468	IC₅₀	> 3 μM Compound: PD-0332991	Antiproliferative activity against Rb-negative human MDA-MB-468 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis Antiproliferative activity against Rb-negative human MDA-MB-468 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis	[PMID: 26115571]
MDA-MB-468	IC₅₀	> 3 μM Compound: 43(table 3)	Inhibitory concentration was measured by the incorporation of [14C]thymidine in (human breast carcinoma) MDA-MB-468 cell line Inhibitory concentration was measured by the incorporation of [14C]thymidine in (human breast carcinoma) MDA-MB-468 cell line	[PMID: 15801831]
MDA-MB-468	EC₅₀	1.9 μM Compound: Palbociclib	Growth inhibition of human MDA-MB-468 cells measured after 72 hrs by propidium iodide staining based fluorescence assay Growth inhibition of human MDA-MB-468 cells measured after 72 hrs by propidium iodide staining based fluorescence assay	[PMID: 30665142]
MDA-MB-468	GI₅₀	5.96 μM Compound: Palbociclib	Growth inhibition of human MDA-MB-468 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human MDA-MB-468 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
MDA-MB-468	IC₅₀	5424 nM Compound: Palbociclib	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay	[PMID: 32200202]
MIA PaCa-2	IC₅₀	10.6 μM Compound: Palbociclib	Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth by MTT assay	[PMID: 33316409]
MM1.S	IC₅₀	200 nM Compound: PD	Antiproliferative activity against human MM1S cells after 84 hrs by CCK8 assay Antiproliferative activity against human MM1S cells after 84 hrs by CCK8 assay	[PMID: 31330105]
MOLM-13	IC₅₀	> 3 μM Compound: Palbociclib	Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as inhibition of STAT5 phosphorylation at Tyr694 after 24 hrs Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as inhibition of STAT5 phosphorylation at Tyr694 after 24 hrs	[PMID: 24641103]
MOLM-13	GI₅₀	> 80 μM Compound: Palbociclib	Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay	[PMID: 34958208]
MOLM-13	IC₅₀	0.011 μM Compound: Palbociclib	Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs	[PMID: 24641103]
MOLM-13	GI₅₀	0.062 μM Compound: Palbociclib	Growth inhibition of human MOLM13 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human MOLM13 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
MOLM-13	IC₅₀	0.096 μM Compound: Palbociclib	Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis	[PMID: 24641103]
MOLM-13	IC₅₀	0.096 μM Compound: Palbociclib	Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis	[PMID: 24641103]
MRC5	GI₅₀	> 10 μM Compound: Palbociclib	Growth inhibition of human MRC5 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human MRC5 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
MV4-11	GI₅₀	0.05 μM Compound: Palbociclib	Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay	[PMID: 28156111]
NB-4	GI₅₀	0.066 μM Compound: Palbociclib	Growth inhibition of human NB4 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human NB4 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
NCI-H1299	IC₅₀	8.92 μM Compound: PD0332991	Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33857728]
OVCAR-3	IC₅₀	> 3 μM Compound: 1	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 6 days by CyQuant assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 6 days by CyQuant assay	[PMID: 34110834]
PC-3	GI₅₀	0.071 μM Compound: Palbociclib	Growth inhibition of human PC3 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human PC3 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
PC-3	IC₅₀	2.2 μM Compound: V	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: 30572179]
Raji	GI₅₀	30 μM Compound: Palbociclib	Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
RPMI-8226	GI₅₀	2.215 μM Compound: Palbociclib	Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
Sf9	IC₅₀	> 10 μM Compound: Palbociclib	Inhibition of human full length N-terminal GST-fused CDK2 (M1 to L298 residues)/human full length Cyclin-A2 (M1 to L432 residues) expressed in Sf9 cells using histone H1 as substrate measured after 1 hr by ADP-glo luminescence assay Inhibition of human full length N-terminal GST-fused CDK2 (M1 to L298 residues)/human full length Cyclin-A2 (M1 to L432 residues) expressed in Sf9 cells using histone H1 as substrate measured after 1 hr by ADP-glo luminescence assay	[PMID: 30665142]
Sf9	IC₅₀	> 10 μM Compound: Palbociclib	Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	> 10 μM Compound: Palbociclib	Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	> 100 μM Compound: Palbociclib	Inhibition of recombinant human N-terminal GST/His6-tagged CDK1 (M1 to M297 residues)/CyclinB1 (M1 to V433 residues) expressed in Sf9 insect cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay Inhibition of recombinant human N-terminal GST/His6-tagged CDK1 (M1 to M297 residues)/CyclinB1 (M1 to V433 residues) expressed in Sf9 insect cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay	[PMID: 30665142]
Sf9	IC₅₀	> 100 μM Compound: Palbociclib	Inhibition of N-terminal GST-HIS6 fusion protein tagged human full length CDK9 (M1 to F372 residues)/N-terminal HIS6-fused human Cyclin-T1 (M1 to K726 residues) expressed in Sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence as Inhibition of N-terminal GST-HIS6 fusion protein tagged human full length CDK9 (M1 to F372 residues)/N-terminal HIS6-fused human Cyclin-T1 (M1 to K726 residues) expressed in Sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence as	[PMID: 30665142]
Sf9	IC₅₀	0.005 μM Compound: Palbociclib	Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay	[PMID: 32129996]
Sf9	IC₅₀	0.013 μM Compound: Palbociclib	Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay	[PMID: 30665142]
Sf9	IC₅₀	0.013 μM Compound: Palbociclib	Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	1.1 μM Compound: Palbociclib	Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	1.207 μM Compound: Palbociclib	Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay	[PMID: 32129996]
Sf9	IC₅₀	8.75 μM Compound: Palbociclib	Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay	[PMID: 32129996]
Sf9	IC₅₀	9.1 μM Compound: Palbociclib	Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	9.2 μM Compound: PD-0332991	Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP	[PMID: 26851505]
Sf9	IC₅₀	9.8 μM Compound: Palbociclib	Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
SK-MEL19	GI₅₀	30 μM Compound: Palbociclib	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]
T47D	EC₅₀	0.35 μM Compound: Palbociclib	Growth inhibition of human T47D cells measured after 72 hrs by propidium iodide staining based fluorescence assay Growth inhibition of human T47D cells measured after 72 hrs by propidium iodide staining based fluorescence assay	[PMID: 30665142]
T47D	GI₅₀	1.056 μM Compound: Palbociclib	Antiproliferative activity against human T47D cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human T47D cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36350721]
U-266	GI₅₀	11.274 μM Compound: Palbociclib	Antiproliferative activity against human U-266 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human U-266 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
U-87MG ATCC	IC₅₀	345.2 nM Compound: Palbociclib	Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay	[PMID: 32200202]
U-937	IC₅₀	0.14 μM Compound: Palbociclib	Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis	[PMID: 24641103]
ZR-75-1	GI₅₀	2.279 μM Compound: Palbociclib	Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36350721]

体外研究
(In Vitro)

Palbociclib (0-1 μM，24 h) 抑制 MDA-MB-435 细胞中 Ser⁷⁹⁵ 位点的 Rb 磷酸化，IC₅₀ 值为 0.063 μM，并获得相似的效果对 Colo -205 结肠癌中 Ser⁷⁸⁰ 和 Ser⁷⁹⁵ 磷酸化的影响^[1]。
Palbociclib (0-10 μM，24 h) 仅在 G1 期抑制 MDA-MB-453 细胞^[1]。
Palbociclib (500 nM，7 天) 增加同源基因 (H2d1、H2k1 和 B2m) 的表达) 在 MDA-MB-453 和 MDA-MB-361 细胞中^[2]。
Palbociclib (0-1 μM，6 天) 抑制多种管腔 ER 阳性细胞和HER2 扩增的乳腺癌细胞系，IC₅₀ 值范围为 4 nM 至 1 μM^[3]。
Palbociclib (0-1 μM，3 天) 抑制人肝癌细胞系的增殖，IC₅₀ 值范围为 0.01 μM 至 3.49 μM，并诱导可逆的细胞周期停滞^[4]。

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

Cell Cycle Analysis^[1]

Cell Line:	MDA-MB-453 cells
Concentration:	0-1 μM
Incubation Time:	24 h
Result:	Arrested MDA-MB-453 cells in G1.

Cell Proliferation Assay^[3]

Cell Line:	ER-positive as well as HER2-amplified breast cancer cell lines (MDA-MB-175, ZR-75-30, CAMA-1, etc.)
Concentration:	0-1 μM
Incubation Time:	6 days
Result:	Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines.

体内研究
(In Vivo)

Palbociclib (口服，75 或 150 mg/kg，每日一次，持续 14 天) 可使肿瘤快速消退并延缓肿瘤生长^[1]。
Palbociclib (口服，90 mg/kg，每日一次，持续 12 天) 减少无肿瘤小鼠脾脏和淋巴结中的 Treg 数量和 Treg:CD8 比率，证明了肿瘤非依赖性效应^[2]。
Palbociclib (口服，100 mg/kg，daily for 1 week) 对肝癌基因工程镶嵌小鼠模型具有有效的抗肿瘤作用^[4]。

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

Animal Model:	Mice bearing Colo-205 colon carcinoma xenografts (p16 deleted)^[1]
Dosage:	75, 150 mg/kg, daily for 14 days
Administration:	Oral adminstration
Result:	Produced rapid tumor regressions and a corresponding tumor growth delay of ~50 days.

Animal Model:	Tumor-free female FVB mice^[2]
Dosage:	90 mg/kg (diluted in 50 nM sodium D-lactate), daily for 12 days
Administration:	Oral adminstration
Result:	Reduced total thymic mass and immature CD4⁺ and CD8⁺ double-positive thymocytes, and increased the fractions of CD4⁺ and CD8⁺ single-positive thymocytes.

Animal Model:	Genetically engineered mosaic mouse model of liver cancer (Myc;p53-sgRNA)^[4]
Dosage:	100 mg/kg, daily for 1 week.
Administration:	Oral adminstration
Result:	Decreased the luminescence signal in liver and delayed tumour growth.

Clinical Trial

分子量

447.53

Formula

C₂₄H₂₉N₇O₂

CAS 号

571190-30-2

性状

固体

颜色

Light yellow to yellow

中文名称

帕布昔利布；帕博西尼；哌柏西利；帕柏西利；帕博昔布；帕博赛布；哌泊塞克雷；帕布西利布；帕布昔里布；帕布西里布

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

细胞实验：

0.1 M HCL 中的溶解度 : 25 mg/mL (55.86 mM; ultrasonic and adjust pH to 4 with 0.1 M HCL)

DMSO 中的溶解度 : 5 mg/mL (11.17 mM; ultrasonic and adjust pH to 5 with HCl; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2345 mL	11.1724 mL	22.3449 mL
5 mM	0.4469 mL	2.2345 mL	4.4690 mL
10 mM	0.2234 mL	1.1172 mL	2.2345 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, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1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 mg/mL (4.47 mM); 澄清溶液

此方案可获得 ≥ 2 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 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 mg/mL (4.47 mM); 澄清溶液

此方案可获得 ≥ 2 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 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。
20% SBE-β-CD in Saline 的配制（4°C，储存一周）：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。

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： 15% Cremophor EL 85% Saline
Solubility: 25 mg/mL (55.86 mM); 悬浊液; 超声助溶
方案二

请依序添加每种溶剂： 0.5% CMC/saline water
Solubility: 6.67 mg/mL (14.90 mM); 悬浊液; Need ultrasonic and warming and heat to 42°C

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）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.94%

选择批次：

Data Sheet (650 KB) SDS (623 KB)

COA (289 KB) HNMR (207 KB) RP-HPLC (184 KB) MS (69 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38. [Content Brief]

[2]. Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475. [Content Brief]

[3]. Richard S Finn, et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009;11(5):R77. [Content Brief]

[4]. Bollard J, et al. Palbociclib (PD-0332991), a selective CDK4/6 inhibitor, restricts tumour growth in preclinical models of hepatocellular carcinoma. Gut. 2017 Jul;66(7):1286-1296. [Content Brief]

Palbociclib 相关分类

Cancer

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 / 0.1 M HCL	1 mM	2.2345 mL	11.1724 mL	22.3449 mL	55.8622 mL
	5 mM	0.4469 mL	2.2345 mL	4.4690 mL	11.1724 mL
	10 mM	0.2234 mL	1.1172 mL	2.2345 mL	5.5862 mL
0.1 M HCL	15 mM	0.1490 mL	0.7448 mL	1.4897 mL	3.7241 mL
	20 mM	0.1117 mL	0.5586 mL	1.1172 mL	2.7931 mL
	25 mM	0.0894 mL	0.4469 mL	0.8938 mL	2.2345 mL
	30 mM	0.0745 mL	0.3724 mL	0.7448 mL	1.8621 mL
	40 mM	0.0559 mL	0.2793 mL	0.5586 mL	1.3966 mL
	50 mM	0.0447 mL	0.2234 mL	0.4469 mL	1.1172 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.

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Palbociclib (Synonyms: 帕博西尼; PD 0332991)

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参考文献

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Palbociclib (Synonyms: 帕博西尼; PD 0332991)

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摩尔计算器

稀释计算器

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