AMG-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AMG-1是人RON和c-Met的有效抑制剂。体外激酶测定表明，化合物I是人RON和c-Met的有效抑制剂，IC50分别为9和4 nmol/L。

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.

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.

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.

RON-IN-1 | SYN1143

Angiogenesis

c-Met/HGFR

c-Met|RON

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913376-84-8

556.58

C31H29FN4O5

>98% (HPLC)

DMSO:90 mg/mL?(161.7 mM;?Need ultrasonic)

CC(C)(CN(C(C)=C(C(Nc(cc1)cc(F)c1Oc1ccnc2cc(OC)ccc12)=O)C1=O)N1c1ccccc1)O

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(-20℃)

With Ice Pack

≥ 2 years