MRTX-EX185 | KRAS inhibitor | Probechem Biochemicals

Chemical Structure : MRTX-EX185

CAS No.: 2621927-57-7

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MRTX-EX185 (EX185)

货号: PC-38438Not For Human Use, Lab Use Only.

MRTX-EX185 (EX185) is a novel potent small-molecule inhibitor of KRAS mutants, exhibits target engagement against KRAS (G12D) with IC50 of 90 nM, binds to GDP-loaded KRAS and KRAS(G12D), as well as the active GNP state.

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5 mg	￥3580	In stock
10 mg	￥5580	In stock
25 mg	￥8980	In stock
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生物&药学活性

MRTX-EX185 (EX185) is a novel potent small-molecule inhibitor of KRAS mutants, exhibits target engagement against KRAS (G12D) with IC50 of 90 nM, binds to GDP-loaded KRAS and KRAS(G12D), as well as the active GNP state.
MRTX-EX185 also bound GDP-loaded HRAS.
MRTX-EX185 engages both nucleotide states-albeit with preference for the inactive GDP-loaded protein-and might present an opportunity to inhibit even constitutively active (GTP-loaded) KRAS hotspot mutants
MRTX-EX185 engages numerous KRAS Q61, G12 and G13 mutant proteins and drives antiproliferation.

物理化学性质&存储条件

分子量	564.665
分子式	C33H33FN6O2
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	4-[4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)pyrido[4,3-d]pyrimidin-7-yl]-5-ethynylnaphthalen-2-ol

参考文献

1. James D Vasta, et al. Nat Chem Biol. 2022 Mar 21. doi: 10.1038/s41589-022-00985-w.

MRTX-EX185 (EX185)

生物&药学活性

物理化学性质&存储条件

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MRTX-EX185 (EX185)

生物&药学活性

物理化学性质&存储条件

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