TSN084 | Multikinase inhibitor | Probechem Biochemicals

Chemical Structure : TSN084

TSN084 (TSN 084, TSN-084)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt	596.59
Formula	C32H26F2N6O4
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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

References

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

2. WO2020048455 A1.

TSN084 (TSN 084, TSN-084)

Biological Activity

Physicochemical Properties

References

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