Palbociclib hydrochloride

Research use only, not for human use.

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.

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.

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:0-10 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 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 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)Dosage:100 mg/kg, daily for 1 week.Administration:Oral adminstrationResult:Decreased the luminescence signal in liver and delayed tumour growth.

PD-0332991 hydrochloride | PD0332991 hydrochloride | PD 0332991 hydrochloride

Cell Cycle/DNA Damage

CDK

CDK2/CyclinA|CDK2/CyclinE2|CDK4/CyclinD1|CDK4/CyclinD3|CDK6/CyclinD2

Cancer

Breast Cancer

827022-32-2

483.9937

C24H30ClN7O2

>98% (HPLC)

DMSO: 6 mg/mL (Need ultrasonic or warming)

Cl.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]-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years