MRTX-1257

SKU: orb1308008

Description

MRTX-1257 is a potent, covalent, and selective KRAS G12C inhibitor with an IC50 of 900 pM in cellular assays. It demonstrates good oral bioavailability in mice and achieves significant in vivo target engagement, supporting its use in both in vitro mechanistic studies and in vivo efficacy models for KRAS-driven cancers.

Research Area

Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 2206736-04-9
• MW: 565.71
• Purity: 99.07% (May vary between batches)
• Formula: C₃₃H₃₉N₇O₂
• SMILES: CN1CCC[C@H]1COc1nc2CN(CCc2c(n1)N1CCN([C@@H](CC#N)C1)C(=O)C=C)c1cccc2cccc(C)c12
• Target: Ras,Kras
• Solubility: DMSO:35 mg/mL (61.87 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.54 mM)

Bioactivity

• In Vivo:
  MRTX-1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose groups. MRTX-1257 dosed of 100 mg/kg daily causes complete responses that are maintained >70 days after cessation of treatment. MRTX-1257 (1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg, orally, daily for 30 days) displays rapid tumor growth inhibition at all dose groups in MIA PaCa-2 G12C Xenograft model in mice .
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Storage & Handling

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

Alternative Names

covalent, cancer, ERK, G12C, H358 cells, inhibit, irreversible, mutant, MRTX1257, MRTX-1257, MRTX 1257, KRAS, KRAS(G12C), KRAS G12C, Inhibitor, selective, phosphorylation, Ras

Compound Identifiers

PubChem CID

134326084