化合物Dalpiciclib T9636

Product Introduction
Bioactivity


英文名: Dalpiciclib

描述: 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。

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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 3.5 mg/mL (7.84 mM)


关键字: MCF7 | BT-474/T | Cyclin dependent kinase | Eca 109 | MCF7/TR | and KYSE-510 ESCC | Dalpiciclib | Inhibitor | inhibit | Eca 9706 | antitumor activity | SHR 6390 | CDK | SHR6390

相关产品: MLS-573151 | ML167 | SCH900776 | BUR1 | Atuveciclib | 5-Iodo-indirubin-3'-monoxime | Cdc7-IN-5 | bio-THZ1 | GP-82996 | Dinaciclib

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Clinical Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | Highly Selective Inhibitor Library

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