AMG410

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].

Product Specifications

CAS Number

[3040175-17-2]

UNSPSC

12352005

Target

Ras

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Purity

99.75

Solubility

DMSO : 4 mg/mL (ultrasonic; warming; heat to 60°C)

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

Molecular Formula

C31H32ClF2N7O5

Molecular Weight

656.08

References & Citations

[1]Adriano BAUER, et al. Macrocyclic kras inhibitors and methods of use. WO2024107686A1.|[2]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