Pan-Trk-IN-3

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Pan-Trk-IN-3 

Pan-Trk-IN-3 (Compound 11g) 是一种有效的广谱 Trk 及其耐药突变体抑制剂。对 TrkATrkBTrkCTrkAG595RTrkAG667CTrkAG667STrkAF589LTrkCG623RIC50 分别为 2、3、2、21、26、5、7 和 6 nM。Pan-Trk-IN-3 表现出极好的抗肿瘤活性,诱导细胞凋亡 (apoptosis)。

Pan-Trk-IN-3

Pan-Trk-IN-3 Chemical Structure

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生物活性

Pan-Trk-IN-3 (Compound 11g) is a potent inhibitor of pan-Trk and their drug-resistant mutants with IC50 values of 2, 3, 2, 21, 26, 5, 7 and 6 nM against TrkA, TrkB, TrkC, TrkAG595R, TrkAG667C, TrkAG667S, TrkAF589L and TrkCG623R, respectively. Pan-Trk-IN-3 displays excellent antitumor activity and induces apoptosis[1].

IC50 & Target

TrkA

2 nM (IC50)

TrkC

2 nM (IC50)

TrkB

3 nM (IC50)

TrkAG667S

5 nM (IC50)

TrkCG623R

6 nM (IC50)

TrkAF589L

7 nM (IC50)

TrkAG595R

21 nM (IC50)

TrkAG667C

26 nM (IC50)

分子量

575.06

Formula

C29H31ClN8O3

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.

参考文献
  • [1]. Pan S,et al. Structural Optimization and Structure-Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)-6H-pyrimido[5,4-b][1,4]oxazin-7(8H)-one Derivatives as A New Class of Potent Inhibitors of Pan-Trk and Their Drug-Resistant Mutants. J Med Chem. 2022 Feb 10;65(3):2035-2058.

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