AMG-1

SKU: orb1217485

Description

AMG-1 is a potent inhibitor of human RON and c-Met.In vitro kinase assays showed that compound I is a potent inhibitor of human RON and c-Met with IC50s of 9 and 4 nmol/L, respectively.

Key Properties

• CAS Number: 913376-84-8
• MW: 556.58
• Purity: >98% (HPLC)
• Formula: C₃₁H₂₉FN₄O₅
• SMILES: CC(C)(CN(C(C)=C(C(Nc(cc1)cc(F)c1Oc1ccnc2cc(OC)ccc12)=O)C1=O)N1c1ccccc1)O
• Target: c-Met/HGFR
• Solubility: DMSO:90 mg/mL (161.7 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  SYN1143 (10-100 mg/kg; p.o. for 22 d) inhibits the growth of c-Met-dependent and constitutively active RON-expressing tumors in mice. SYN1143 (20-50 μg; transferred into calvarial defects) stimulates bone formation in critical-sized defects of mouse calvarial bone. Animal model: Female CD1 nu/nu mice (6-8 weeks) bearing NIH3T3 TPR-Met s. c. tumors. Dosage: 10, 30, 100 mg/kg. Administration: Oral gavage either once or twice daily for 22 days. Result: Significantly inhibited tumor growth at doses of 30 or 100 mg/kg once daily or at 30 mg/kg twice daily. Completely inhibited tumor growth at a dose of 100 mg/kg once daily.
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• In Vitro:
  SYN1143 (Compound I) (10-1000 nM; 1 h) inhibits c-Met-mediated signaling and functional activity in HT-29 and BxPC3 cells. SYN1143 (10-1000 nM; 1 h) inhibits RON-mediated signaling and functional activity in NIH3T3 RON and BxPC3 cells. SYN1143 (0.3-30 μM; 2 h or 3 d) inhibits c-Met signaling and cell proliferation in MC3T3-E1 and C3H10T1/2 cells. SYN1143 (0.3-2 μM; 4-12 d) potentiates osteogenic differentiation of precursor cells. Western blot analysis. Cell line: HT-29 and BxPC3 cells. Concentration: 10, 30, 100, 300, 1000 nM. Incubation time: 1 hours. Result: Inhibited HGF-mediated c-Met phosphorylation and downstream signaling in a dose-dependent manner in both cell lines.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RON-IN-1 | SYN1143

Quick Database Links

Gene Symbol

c-Met/HGFR