Palbociclib (PD 0332991) dihydrochloride 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 dihydrochloride 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。

Palbociclib (PD 0332991) dihydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC 50 values of 11 and 16 nM, respectively. Palbociclib dihydrochloride 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].

Palbociclib dihydrochloride (0-1 μM, 24 h) inhibits Rb Phosphorylation at Ser 795 in MDA-MB-435 cells with an IC 50 value of 0.063 μM, and obtains similar effects on both Ser 780 and Ser 795 phosphorylation in the Colo-205 colon carcinoma [1]. Palbociclib dihydrochloride (0-10 μM, 24 h) arrests MDA-MB-453 cells exclusively in G1 phase [1]. Palbociclib dihydrochloride (500 nM, 7 days) increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells [2]. Palbociclib dihydrochloride (0-1 μM, 6 days) inhibits growth of several luminal ER-positive as well as HER2-amplified breast cancer cell lines, with IC 50 values ranging from 4 nM to 1 μM [3]. Palbociclib dihydrochloride (0-1 μM, 3 days) inhibits the proliferation of human liver cancer cell lines with IC 50 values ranging from 0.01 μM to 3.49 μM, and induces a reversible cell cycle arrest [4]. 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: 0-10 μM Incubation Time: 6 days Result: Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines.

Palbociclib dihydrochloride (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth [1]. Palbociclib dihydrochloride (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 [2]. Palbociclib dihydrochloride (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer [4]. 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.

C24H31Cl2N7O2

520.45

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years