Dalpiciclib - CAS:1637781-04-4

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Dalpiciclib (Synonyms:SHR-6390)

目录号 : KM9918 CAS No. : 1637781-04-4

Data Sheet 产品使用指南

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。

规格	价格	是否有货	数量
5mg		In-stock
10mg		In-stock
25mg		In-stock

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生物活性

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.

体外研究

Dalpiciclib (SHR-6390) (0-4 μM) inhibits cell proliferation in a dose-dependent manner.
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.

Cell Proliferation Assay

Cell Line:	Eca 109, Eca 9706, and KYSE-510 ESCC cell lines
Concentration:	0-4 μM
Incubation Time:	72 hours
Result:	Inhibited cell proliferation in a dose-dependent manner, with Eca 109 being the relative sensitive one and Eca 9706 being the relative resistant one.

体内研究

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

Animal Model:	NOD/SCID mice (ESCC PDXs models)
Dosage:	150 mg/kg
Administration:	Oral gavage; weekly for 3 weeks
Result:	The growth of tumor was significantly suppressed in SHR6390 treatment group with various suppressions.

分子式

C₂₅H₃₀N₆O₂

分子量

446.54

CAS号

1637781-04-4

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.

Data Sheet

产品使用指南

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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