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编 号：F762367
分子式：C24H31Cl2N7O2
分子量：520.45
分子式：C24H31Cl2N7O2
分子量：520.45
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CAS No: 1831842-69-3
产品详情
生物活性：
Palbociclib (PD 0332991) dihydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 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.
体内研究：
Palbociclib dihydrochloride (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth.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.Palbociclib dihydrochloride (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer.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 adminstration
Result:Decreased the luminescence signal in liver and delayed tumour growth.
体外研究：
Palbociclib dihydrochloride (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 dihydrochloride (0-10 μM, 24 h) arrests MDA-MB-453 cells exclusively in G1 phase.Palbociclib dihydrochloride (500 nM, 7 days) increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells.Palbociclib dihydrochloride (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 dihydrochloride (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.
Palbociclib (PD 0332991) dihydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 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.
体内研究：
Palbociclib dihydrochloride (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth.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.Palbociclib dihydrochloride (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer.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 adminstration
Result:Decreased the luminescence signal in liver and delayed tumour growth.
体外研究：
Palbociclib dihydrochloride (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 dihydrochloride (0-10 μM, 24 h) arrests MDA-MB-453 cells exclusively in G1 phase.Palbociclib dihydrochloride (500 nM, 7 days) increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells.Palbociclib dihydrochloride (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 dihydrochloride (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.
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