JNJ-38877618

SKU: orb1308174

Description

JNJ-38877618 (OMO-1) is a potent and selective Met kinase inhibitor, demonstrating low nanomolar IC50 values against both wild-type and mutant forms. It is a valuable research tool for investigating Met-driven oncogenesis in cellular assays and has shown antitumor efficacy in preclinical in vivo models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 943540-74-7
• MW: 374.35
• Purity: 99.74% (May vary between batches)
• Formula: C₂₀H₁₂F₂N₆
• SMILES: FC(F)(c1nnc2ccc(nn12)-c1ccncc1)c1ccc2ncccc2c1
• Target: c-Met/HGFR
• Solubility: DMSO:4.5 mg/mL (12.02 mM)

Bioactivity

• Target IC50:
  MET (WT):2 nM|MET (mutant):2 nM
• In Vivo:
  JNJ-38877618 effectively induces regression in substantial Met-amplified EBC-1 SqNSCLC by dose- and time-dependently inhibiting Met kinase activation, with the inhibition lasting significantly longer than its plasma presence. It entirely halts tumor growth in three distinct models: SNU5 Met amp gastric, U87-MG HGF autocrine glioblastoma, and Hs746T Met exon 14 skipping mutant gastric cancer. Additionally, combination therapies are well tolerated and enhance EGFR-targeted treatments.
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• In Vitro:
  JNJ-38877618 shows nM potency against Met Ampl/mutant and therapy-resistant models. JNJ-38877618 has nM binding affinity (Kd=1.4 nM) and enzyme inhibitory activity against wt and M1268T mutant Met (2 and 3 nM IC50). Met inhibitory effects are assessed in proliferation, colony formation, and motility assays.
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Storage & Handling

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

Alternative Names

cMet/HGFR, c-Met/HGFR, cMet, c-Met, Inhibitor, HGFR, inhibit, mutant Met, JNJ 38877618, JNJ38877618, JNJ-38877618, Met, OMO 1, OMO1, OMO-1, wt Met

Compound Identifiers

PubChem CID

57654476