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编 号：F755470
分子式：C29H33N9O6
分子量：603.63
分子式：C29H33N9O6
分子量：603.63
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CAS No: 2757498-64-7
产品详情
生物活性：
Palbociclib (PD 0332991) orotate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
体内研究：
Palbociclib (oral adminstration, 75 or 150 mg/kg, daily for 14 days) orotate produces rapid tumor regressions and delays tumor growth.Palbociclib (oral adminstration, 90 mg/kg, daily for 12 days) orotate 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) orotate 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
Administration:Oral administration; daily for 14 days
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
Administration:Oral administration; daily for 12 days
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
Administration:Oral administration; daily for 1 week
Result:Decreased the luminescence signal in liver and delayed tumour growth.
体外研究：
Palbociclib (0-1 μM, 24 h) orotate inhibits retinoblastoma 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) orotate arrests MDA-MB-453 cells exclusively in G1 phase.Palbociclib (500 nM, 7 days) orotate increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells.Palbociclib (0-1 μM, 6 days) orotate 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) orotate 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) orotate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
体内研究：
Palbociclib (oral adminstration, 75 or 150 mg/kg, daily for 14 days) orotate produces rapid tumor regressions and delays tumor growth.Palbociclib (oral adminstration, 90 mg/kg, daily for 12 days) orotate 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) orotate 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
Administration:Oral administration; daily for 14 days
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
Administration:Oral administration; daily for 12 days
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
Administration:Oral administration; daily for 1 week
Result:Decreased the luminescence signal in liver and delayed tumour growth.
体外研究：
Palbociclib (0-1 μM, 24 h) orotate inhibits retinoblastoma 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) orotate arrests MDA-MB-453 cells exclusively in G1 phase.Palbociclib (500 nM, 7 days) orotate increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells.Palbociclib (0-1 μM, 6 days) orotate 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) orotate 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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