Chemical Structure : TSN084
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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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.
分子量 | 596.59 | |
分子式 | C32H26F2N6O4 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Boyu Zhong, et al. Cancer Res (2023) 83 (7_Supplement): 4027.
2. WO2020048455 A1.
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