产品
编 号:F471028
分子式:C26H35N7O6S
分子量:573.66
产品类型
结构图
CAS No: 827022-33-3
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产品详情
生物活性:
Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate 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 isethionate isethionate (口服,75 或 150 mg/kg,每日一次,持续 14 天) 可使肿瘤快速消退并延缓肿瘤生长。 Palbociclib isethionate isethionate (口服,90 mg/kg kg,每日一次,持续 12 天) 减少无肿瘤小鼠脾脏和淋巴结中的 Treg 数量和 Treg:CD8 比率,证明了肿瘤非依赖性效应。 Palbociclib isethionate isethionate (口服给药,100 mg/kg,每日一次,持续 1 周) 在肝癌基因工程镶嵌小鼠模型中具有有效的抗肿瘤作用。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 isethionate dihydrochloride (0-1 μM,24 h) 抑制 MDA-MB-435 细胞中 Ser795 位点的 Rb 磷酸化,IC50 值为 0.063 μM,并获得类似的结果对 Colo -205 结肠癌中 Ser780 和 Ser795 磷酸化的影响。 Palbociclib isethionate dihydrochloride (0-10 μM,24 小时) 仅在 G1 期阻止 MDA-MB-453 细胞。 Palbociclib isethionate dihydrochloride (500 nM,7 天) 增加同源基因的表达 (H2d1、H2k1,和 B2m) 在 MDA-MB-453 和 MDA-MB-361 细胞中。 Palbociclib isethionate dihydrochloride (0-1 μM,6 天) 抑制几种管腔 ER-阳性和 HER2 扩增的乳腺癌细胞系,IC50 值范围为 4 nM-1 μM。 Palbociclib isethionate dihydrochloride (0-1 μM,3 天) 抑制人肝癌细胞系的增殖,IC50 值范围为 0.01 μM 至 3.49 μM,并诱导可逆的细胞周期停滞。