3040175-17-2
Chemical Structure
AMG410
- CAS No.: 3040175-17-2
- Formula:C31H32ClF2N7O5
- Molecular Weight:656.08
InChIKey: FRRZEUVDJRQIGA-QSDPREHASA-N
SMILES: FC1=C(C2=C(C=NN3)C3=CC(Cl)=C2CCCO4)N=CC5=C1N=C(OC[C@]67C[C@@H](F)CN6CCC7)N=C5N8CCOC[C@@H](OC4=O)C8
Biological Activity: AMG410 is a non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 shows greater than 100-fold selectivity against both HRAS and NRAS. AMG410 is a dual GTP(on)- and GDP(off)-state inhibitor (Kd(GDP-state) of 1 nM; Kd(GTP-state) of 22 nM). AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. AMG410 can be used for the study of colorectal, pancreatic, and lung cancers[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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AMG410 | 99.75% | AMG410 is a non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 shows greater than 100-fold selectivity against both HRAS and NRAS. AMG410 is a dual GTP(on)- and GDP(off)-state inhibitor (Kd(GDP-state) of 1 nM; Kd(GTP-state) of 22 nM). AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. AMG410 can be used for the study of colorectal, pancreatic, and lung cancers. | ||||||||||||||||||||
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- [1]. Adriano BAUER, et al. Macrocyclic kras inhibitors and methods of use. WO2024107686A1.
- [2]. Brian A. Lanman, et al. Abstract ND01: AMG 410: An H/NRAS-sparing pan-KRAS inhibitor with dual GTP(on)/GDP(off)-state activity for the treatment of diverse KRAS-mutant tumors. Cancer Res (2025) 85 (8_Supplement_2): ND01.
Keywords
