Capmatinib 2HCl

SKU: orb1303013

Description

Capmatinib 2HCl (INC-280 2HCl) is a highly potent and selective ATP-competitive c-MET kinase inhibitor (IC50=0.13 nM). It blocks c-MET phosphorylation and downstream signaling, inhibiting proliferation and migration while inducing apoptosis in c-MET-dependent cancer cells in vitro, and has shown antitumor efficacy in vivo models.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1197376-85-4
• MW: 485.34
• Purity: 100.00%
• Formula: C₂₃H₁₉Cl₂FN₆O
• SMILES: Cl.Cl.CNC(=O)c1ccc(cc1F)-c1cnc2ncc(Cc3ccc4ncccc4c3)n2n1
• Target: Apoptosis,c-Met/HGFR
• Solubility: DMSO:11 mg/mL (22.66 mM)

Bioactivity

• Target IC50:
  c-Met (cell-free assay):0.13 nM
• In Vivo:
  INCB28060(free base) shows strong antitumor activity in c-MET-dependent mouse tumor models, even oral treatment of 0.03 mg/kg INCB28060 causes approximately 50% inhibition of c-MET-phosphorylation. Dose-dependent inhibition of tumor growth is observed in tumor-bearing mice.
• In Vitro:
  Capmatinib(free base）exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10,000-fold selectivity over a large panel of human kinases. Capmatinib inhibits human c-MET phosphorylation and c-MET-mediated signaling in cancer cells. Capmatinib inhibits c-MET-dependent cell proliferation and survival, and prevents anchorage-independent cancer cell growth and cell migration.
• Cell Research:
  Cell lines: H441 cells. Concentrations: 0.24,1,4,16,63 nM. Incubation Time: 24 hours. Method:H441 cells are seeded in RPMI-1640 medium containing 10% FBS and grown to complete confluence.Gaps are introduced by scraping cells with a P200 pipette tip.Cells are then stimulated with 50 ng/mL recombinant human HGF to induce migration across the gap in the presence of various concentrations of INCB28060.After an overnight incubation,representative photographs are taken and a semiqualitative assessment of inhibition of cell migration is conducted.
• Animal Research:
  Animal Models: Eight-week-old female Balb/c nu/nu mice (Charles River) are inoculated subcutaneously with 4 × 106 tumor cells (S114 model) or with 5 × 106 tumor cells (U-87 mg glioblastoma model). Formulation: INCB28060 is prepared as a 5 mM stock solution in 100% dimethyl sulfoxide and routinely stored at room temperature. Dosages: 3,10,30 mg/kg. Administration: INCB28060 is orally dosed,twice each day.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SNU-5, S114, U-87MG, H441, HGFR, Inhibitor, orally active, inhibit, INCB28060, INCB-28060, INCB28060 2HCl, INC 280, INCB 28060, INC280, INC-280, INC-280 2HCl, c-Met/HGFR, cMet/HGFR, c-Met, cMet, Balb/c nu/nu mice, Capmatinib, Capmatinib 2HCl, Apoptosis, ATP competitive

Compound Identifiers

PubChem CID

44513225