JNJ-38877605

SKU: orb1301078

Description

JNJ-38877605

Research Area

Signal Transduction

Key Properties

• CAS Number: 943540-75-8
• MW: 377.35
• Purity: 98.61% (May vary between batches)
• Formula: C₁₉H₁₃F₂N₇
• SMILES: Cn1cc(cn1)-c1ccc2nnc(n2n1)C(F)(F)c1ccc2ncccc2c1
• Target: c-Met/HGFR
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.65 mM);DMSO:6 mg/mL (15.9 mM)

Bioactivity

• Target IC50:
  c-Met:4 nM
• In Vivo:
  In mice bearing established GTL16 xenografts, JNJ-38877605 (40 mg/kg/day, p.o., total 3day) results in a statistically marked decrease in the plasma levels of human IL-8 (0.150-0.050 ng/mL) and GROα (0.080-0.030 ng/mL). While concentrations of uPAR in the blood become reduced to more than 50% at the same dose.
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• In Vitro:
  JNJ-38877605 shows more than 600-fold selectivity for c-Met compared with more than 200 other diverse tyrosine and serine-threonine kinases and also potently inhibits HGF-stimulated and constitutively activated c-Met phosphorylation in vitro. In EBC1, GTL16, NCI-H1993, and MKN45 cells, JNJ-38877605 (500 nM) leads to a significant reduction of phosphorylation of Met and RON, another key player in invasive growth. A recent study shows that JNJ-38877605 is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells.
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• Animal Research:
  Animal Models: GTL16 cells are inoculated subcutaneously into the right posterior flank (or both right and left posterior flanks,for determination of uPAR and IL-6) of 6-week-old immuno-deficient nu/nu female mice on Swiss CD1 background. Formulation: JNJ-38877605 is dissolved in PBS. Dosages: ≤40 mg/kg/day. Administration: Administered via p.o.
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Storage & Handling

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

Alternative Names

c-Met/HGFR, cMet, cMet/HGFR, c-Met, JNJ 38877605, JNJ38877605, JNJ-38877605, inhibit, HGFR, Inhibitor

Compound Identifiers

PubChem CID

46911863