Palbociclib (PD0332991) Isethionate

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

Palbociclib (PD0332991) Isethionate 是一种高度选择性的 CDK4/6 抑制剂，IC50 为 11 nM/16 nM。

Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

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 daysAdministration: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.

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Angiogenesis

CDK

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

Cancer

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827022-33-3

573.66

C24H29N7O2·C2H6O4S

>98% (HPLC)

Water: 50 mg/mL warmed (87.15 mM)

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

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(-20℃)

With Ice Pack

≥ 2 years