AMG410

SKU: orb2946000

Description

AMG410 is a potent, non-covalent dual-modality inhibitor targeting both GDP- and GTP-bound KRAS with low nanomolar affinity, showing selectivity over HRAS/NRAS. It is effective against multiple KRAS mutants (e.g., G12D, G12V) in vitro and induces tumor regression with reduced p-ERK in vivo cancer models.

Research Area

Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 3040175-17-2
• MW: 656.08
• Purity: 99.84% (May vary between batches)
• Formula: C₃₁H₃₂ClF₂N₇O₅
• 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
• Target: Kras,Ras
• Solubility: DMSO:4 mg/mL (6.1 mM)

Bioactivity

• Target IC50:
  KRAS (G13D): 1-4 nM|KRas (G12D): 1-4 nM|KRas (G12V): 1-4 nM
• In Vitro:
  Method: The inhibitory activity of AMG410 against various KRAS mutants was evaluated, along with its selectivity in different cell types and its binding affinity to KRAS-GTP and KRAS-GDP. Result: AMG410 exhibited potent inhibition of KRAS G12D, G12V, and G13D mutants (IC₅₀ = 1–4 nM), with a median IC₅₀ of 12 nM in KRAS-mutant tumor cells, and showed weak inhibition in non-transformed cells (IC₅₀ > 5 μM), indicating high selectivity. It bound both GTP- and GDP-bound KRAS (KD = 22 nM and 1 nM, respectively), enabling state-independent blockade of KRAS signaling.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AMG 410

Compound Identifiers

PubChem CID

172142898