Chemical Structure : AMG410
CAS No.: 3040175-17-2
Catalog No.: PC-24662Not For Human Use, Lab Use Only.
AMG410 is a potent, non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D,> 100-fold selectivity against both HRAS and NRAS.
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AMG410 is a potent, non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D,> 100-fold selectivity against both HRAS and NRAS.
AMG 410 is a dual GTP(on)- and GDP(off)-state inhibitor (KD(GDP-state) = 1 nM; KD(GTP-state) = 22 nM), enabling blockade of KRAS signaling in a cycling state-independent manner.
AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells.
AMG 410 shows potent antiproliferative activity in KRAS-mutant cells (median IC50 = 12 nM), with no anti-proliferative effects in non-KRAS-transformed cells (median IC50 >5 µM).
M.Wt | 656.09 | |
Formula | C31H32ClF2N7O5 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
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 |
1. Patent WO2024107686A1.
2. AACR Annual Meeting: April 25-30, 2025
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