Palbociclib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 CDK4/6 抑制剂，IC50 为 11 nM/16 nM；对 CDK2A 无抑制作用 (IC50>5 uM)；抑制 MDA-MB453 细胞，IC50 为 0.16 uM。

A potent and selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM; no inhibition for CDK2A (IC50>5 uM); inhibits MDA-MB453 cells with IC50 of 0.16 uM; shows antiproliferative effect against retinoblastoma (Rb)-positive tumor cells in vitro and reduces the phospho-Ser780/Ser795 on the Rb protein; orally bioavailable.Breast Cancer Approved(In Vitro):Palbociclib (0-1 μM, 24 h) inhibits Rb Phosphorylation at Ser795 in MDA-MB-435 cells with an IC50 value of 0.063 μM, and obtains similar effects on both Ser780 and Ser795 phosphorylation in the Colo-205 colon carcinoma.Palbociclib (0-10 μM, 24 h) arrests MDA-MB-453 cells exclusively in G1 phase.Palbociclib (500 nM, 7 days) increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells.Palbociclib (0-1 μM, 6 days) inhibits growth of several luminal ER-positive as well as HER2-amplified breast cancer cell lines, with IC50 values ranging from 4 nM to 1 μM.Palbociclib (0-1 μM, 3 days) inhibits the proliferation of human liver cancer cell lines with IC50 values ranging from 0.01 μM to 3.49 μM, and induces a reversible cell cycle arrest.(In Vivo):Palbociclib (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth.Palbociclib (oral adminstration, 90 mg/kg, daily for 12 days) reduces Treg numbers and the Treg:CD8 ratio in the spleen and lymph nodes in tumor-free mice, demonstrating the tumor-independent effects.Palbociclib (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer.

Cell Cycle Analysis 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 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.

Animal Model:Mice bearing Colo-205 colon carcinoma xenografts (p16 deleted)Dosage:75, 150 mg/kg, daily for 14 daysAdministration:Oral adminstrationResult:Produced rapid tumor regressions and a corresponding tumor growth delay of ~50 days.Animal Model:Tumor-free female FVB miceDosage:90 mg/kg (diluted in 50 nM sodium D-lactate), daily for 12 daysAdministration:Oral adminstrationResult: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)Dosage:100 mg/kg, daily for 1 week.Administration:Oral adminstrationResult:Decreased the luminescence signal in liver and delayed tumour growth.

PD0332991 | PD-0332991 | PD 0332991

Cell Cycle/DNA Damage

CDK

CDK4|CDK6

Cancer

Breast Cancer

571190-30-2

447.5327

C24H29N7O2

>98% (HPLC)

DMSO: 0.2 mg/mL (Need ultrasonic or warming)

CC(=O)C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N3CCNCC3)N=C2N(C2CCCC2)C1=O

Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-

(-20℃)

With Ice Pack

≥ 2 years