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IACS-13909
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。
IACS-13909图片
规格:98%
分子量:377.27
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
IACS-13909 是一种有效的选择性的,具有口服活性的 SHP2 变构抑制剂,其 IC50 为 15.7 nM,Kd 为 32 nM。与其他磷酸酶 (包括 SHP1) 相比,IACS-13909 对 SHP2 的选择性更高。IACS-13909 抑制受体酪氨酸激酶 (RTK)/MAPK 途径的信号传导,并具有抗癌作用。
货号:ajcx33538
CAS:2160546-07-4
分子式:C17H18Cl2N6
分子量:377.27
溶解度:DMSO : 10 mg/mL (26.51 mM; Need ultrasonic)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers[1].

IACS-13909 (10 nM-10 μM; 14 days) treatment potently suppresses the proliferation of wild-type SHP2 and KYSE-520 cells[1].IACS-13909 (1-5 μM; 2 hours) treatment potently suppresses pERK and pMEK levels in wild-type SHP2 and KYSE-520 cells[1].IACS-13909 potently suppresses the proliferation of both the parental cells and NCI-H1975 CS cells in a dose-dependent manner, with similar potency (GI50 ~1 μM). IACS-13909 (0.041-3.3 μM) suppresses pERK in NCI-H1975 CS cells in a dose-dependent manner[1].

IACS-13909 (70 mg/kg; oral administration; daily; for 21 days) treatment potently suppresses tumor growth in mice, with 100% tumor growth inhibition (TGI) observed following 21 days of dosing[1].

[1]. Yuting Sun, et al. Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib. Cancer Res. 2020 Nov 1;80(21):4840-4853.