Theliatinib

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Theliatinib

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。

CAS NO:

1353644-70-8

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议

产品介绍

Theliatinib (HMPL-309) 是一种有效、ATP 竞争性、高度选择性的 EGFR 抑制剂，对 EGFR 及其下游蛋白 AKT 和 ERK 的磷酸化水平具有很强的抑制作用，具有抗肿瘤活性。Theliatinib (HMPL-309) 对野生型 EGFR 的 Ki 和 IC50 值分别为 0.05 nM 和 3 nM，对 EGFR T790M/L858R 突变体的 IC50 值为 22 nM。

Cas No.	1353644-70-8
别名	西利替尼; Xiliertinib; HMPL-309
Canonical SMILES	O=C(N1C[C@]2([H])N(C)CC[C@]2([H])C1)NC3=CC4=C(NC5=CC=CC(C#C)=C5)N=CN=C4C=C3OC
分子式	C₂₅H₂₆N₆O₂
分子量	442.51
溶解度	DMSO: 5 mg/mL (11.30 mM)
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	Theliatinib (HMPL-309) is a potent, ATP-competitive and highly selective EGFR inhibitor, significantly inhibits phosphorylation of EGFR (p-EGFR) and its downstream targets, AKT and ERK (p-AKT and p-ERK), with anti-tumor activity. Theliatinib (HMPL-309) shows a Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively[1]. [1]. Ren Y, et al. Anti-tumor efficacy of theliatinib in esophageal cancer patient-derived xenografts models with epidermal growth factor receptor (EGFR) overexpression and gene amplification. Oncotarget. 2017 Apr 19;8(31):50832-50844.