Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dalpiciclib (SHR-6390) 是一种高选择性、口服生物利用度和相当效力的 CDK4 和 CKD6 抑制剂,IC50 分别为 12.4 nM 和 9.9 nM。它通过抑制磷酸化 Rb 蛋白和诱导 G1 细胞周期阻滞在食管鳞状细胞癌中发挥有效的抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,560 | 现货 | ||
5 mg | ¥ 3,820 | 现货 | ||
10 mg | ¥ 5,950 | 现货 | ||
25 mg | ¥ 8,830 | 现货 | ||
50 mg | ¥ 11,900 | 现货 | ||
100 mg | ¥ 16,300 | 现货 |
产品描述 | Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable, and comparable potency inhibitor of CDK4 and CKD6 with IC50s of 12.4 nM and 9.9 nM, respectively. Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest. |
靶点活性 | CDK4:12.4 nM, CDK6:9.9 nM |
体外活性 | Dalpiciclib inhibits cell proliferation in a dose-dependent manner following administration of 0-4 μM for 72?hours[2].In the relative sensitive Eca 109 and KYSE-510 cell lines, Dalpiciclib significantly blocks Rb phosphorylation at serine 780 after 24 hours of administration and induces cell cycle arrest but not in relative resistant Eca 9706 cell line[2]. |
体内活性 | Dalpiciclib administered at 150 mg/kg weekly for 3 weeks by oral gavage has antitumor activity in ESCC xenografts[2]. Dalpiciclib in combination with Paclitaxel or Cisplatin provides synergistic inhibition in ESCC xenografts[2]. |
别名 | SHR-6390 |
分子量 | 446.54 |
分子式 | C25H30N6O2 |
CAS No. | 1637781-04-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 3.5 mg/mL (7.84 mM), ultrasonic, adjust pH to 5 with HCl and heat to 60°C
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2394 mL | 11.1972 mL | 22.3944 mL | 55.986 mL |
5 mM | 0.4479 mL | 2.2394 mL | 4.4789 mL | 11.1972 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Dalpiciclib 1637781-04-4 Cell Cycle/Checkpoint CDK MCF7 BT-474/T Cyclin dependent kinase Eca 109 MCF7/TR and KYSE-510 ESCC Inhibitor inhibit Eca 9706 antitumor activity SHR 6390 SHR6390 SHR-6390 inhibitor