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首页-小分子抑制剂&激动剂-Tyrosine Kinase-FLT3-TSN084
TSN084

Chemical Structure : TSN084

CAS No.: 2412309-60-3

TSN084 (TSN 084, TSN-084)

货号: PC-21565Not For Human Use, Lab Use Only.

TSN084 (TSN 084) is a unique small molecule multi-kinase inhibitor of drug-resistant mutations of c-Met, Trks, and Flt3, also inhibits other oncotargets including Axl, DDRs, and CDK8/19.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

TSN084 (TSN 084) is a unique small molecule multi-kinase inhibitor of drug-resistant mutations of c-Met, Trks, and Flt3, also inhibits other oncotargets including Axl, DDRs, and CDK8/19.
TSN084 is a multi-kinase inhibitor, shows >50% inhibition at 0.1 uM for 33 kinases in a panel of 468 kinases, including many oncotargets and their mutants such as Met, Met-Y1235D, Met-M1250T, Flt3, Flt3-N841I, Flt3-ITD, Flt3-K663Q, Flt3-D835Y, Flt3-D835V, Axl, TrkA, DDR1, and CDK8/19.
TSN084 demonstrated potent anti-proliferation activity against many tumor cell lines, e.g. KM12, MKN45, MV-4-11, and HS746T.
TSN084 also effectively inhibited tumor growth in several CDX drug-resistant models like NTRK-G667C and NTRK3-G696C and showed outstanding survival advantage.
TSN084 is an orally bioavailable small molecule agent in mouse, rat, dog, and monkey.

物理化学性质&存储条件

分子量 596.59
分子式 C32H26F2N6O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(3-fluoro-4-((1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl)oxy)phenyl)-1-(4-fluorophenyl)-6-isopropoxy-2-oxo-1,2-dihydropyridine-3-carboxamide

参考文献

1. Boyu Zhong, et al. Cancer Res (2023) 83 (7_Supplement): 4027.

2. WO2020048455 A1.

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