AMG410 - CAS 3040175-17-2

AMG410 is a non-covalent, dual-modality KRAS inhibitor effective against both GDP (OFF) and GTP (ON) binding, with Kd (GDP) of 1 nM and Kd (GTP) of 22 nM, capable of blocking KRAS independently of the cell cycle. AMG410 does not affect HRAS and NRAS2, and exhibits high potency against KRAS G12D, G12V, G12C, G13D, and other mutants, with an IC50 of 1–4 nM. It induces tumour regression and reduces phosphorylated ERK levels in KRAS-mutant cancer models.

Kras, Ras

GPCR/G Protein, MAPK

3040156

0.9984

C31H32ClF2N7O5

656.08

FC=1C=2C=3C4=C(C=C(Cl)C3CCCOC(=O)O[C@]5(CN(C=6C(C1N=C(OC[C@@]78N(C[C@H](F)C7)CCC8)N6)=CN2)CCOC5)[H])NN=C4

-20°C

Ice Packs

Small Compound