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Dalpiciclib
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Dalpiciclib图片
CAS NO:1637781-04-4
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
Dalpiciclib (SHR-6390) 是一种高选择性、口服生物利用度的 CDK4/6 抑制剂，对 CDK4 (IC50=12.4 nM) 和CDK6 (IC50=9.9 nM) 的数值相当。SHR6390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。
Cas No.1637781-04-4
别名SHR-6390
分子式C25H30N6O2
分子量446.54
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable CDK4/6 inhibitor with comparable potencies against CDK4 (IC50=12.4 nM) and CDK6 (IC50=9.9 nM). Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest[1][2].

Dalpiciclib (SHR-6390) (0-4 μM) inhibits cell proliferation in a dose-dependent manner[2].Dalpiciclib (24 hours) significantly blocks phosphorylation of Rb at serine 780 in relative sensitive Eca 109 and KYSE-510 cell lines, but not in relative resistant Eca 9706 cell line.Dalpiciclib induces cell cycle arrest at G1 phase in Eca 109 and KYSE-510 cell lines[2].

Dalpiciclib (SHR-6390) (150 mg/kg; oral gavage; weekly for 3 weeks) shows antitumor activity against ESCC xenografts[2].Dalpiciclib combines with Paclitaxel (PTX) or Cisplatin (CDDP) offered synergistic inhibitory effects in ESCC xenografts[2].

[1]. Zhang P, et al. A phase 1 study of dalpiciclib, a cyclin-dependent kinase 4/6 inhibitor in Chinese patients with advanced breast cancer. Biomark Res. 2021;9(1):24. Published 2021 Apr 12.
[2]. Wang J, et al. CDK4/6 inhibitor-SHR6390 exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated Rb and inducing G1 cell cycle arrest. J Transl Med. 2017;15(1):127. Published 2017 Jun 2.