Palbociclib (PD 0332991) orotate 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 orotate 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。
| 生物活性 | Palbociclib (PD 0332991) orotate is an orally active selectiveCDK4andCDK6inhibitor withIC50values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and inducescell cycle arrestincancercells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breastcancerand hepatocellular carcinoma[1][3][4]. |
| IC50& Target[1] | Cdk4/cyclin D3 9 nM (IC50) | Cdk4/cyclin D1 11 nM (IC50) | Cdk6/cyclin D2 16 nM (IC50) | DYRK1A 2000 nM (IC50) | MAPK 8000 nM (IC50) |
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体外研究
(In Vitro) | Palbociclib (0-1 μM, 24 h) orotate inhibits retinoblastoma phosphorylation at Ser795in MDA-MB-435 cells with an IC50value of 0.063 μM, and obtains similar effects on both Ser780and Ser795phosphorylation in the Colo-205 colon carcinoma[1].
Palbociclib (0-10 μM, 24 h) orotate arrests MDA-MB-453 cells exclusively in G1 phase[1].
Palbociclib (500 nM, 7 days) orotate increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells[2].
Palbociclib (0-1 μM, 6 days) orotate inhibits growth of several luminal ER-positive as well as HER2-amplified breast cancer cell lines, with IC50values ranging from 4 nM to 1 μM[3].
Palbociclib (0-1 μM, 3 days) orotate inhibits the proliferation of human liver cancer cell lines with IC50values ranging from 0.01 μM to 3.49 μM, and induces a reversible cell cycle arrest[4].
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: | 0-1 μM | | Incubation Time: | 6 days | | Result: | Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines. |
Cell Cycle Analysissup>[1] | Cell Line: | MDA-MB-453 cells | | Concentration: | 0-1 μM | | Incubation Time: | 24 h | | Result: | Arrested MDA-MB-453 cells in G1. |
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体内研究
(In Vivo) | Palbociclib (oral adminstration, 75 or 150 mg/kg, daily for 14 days) orotate produces rapid tumor regressions and delays tumor growth[1].
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[2].
Palbociclib (oral administration, 100 mg/kg, daily for 1 week) orotate 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 | | 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[2] | | 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)[4] | | Dosage: | 100 mg/kg | | Administration: | Oral administration; daily for 1 week | | Result: | Decreased the luminescence signal in liver and delayed tumour growth. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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