SYN1143 |
| Catalog No.GC62268 |
SYN1143은 각각 4 및 9 nM의 IC50으로 c-Met/RON의 강력하고 선택적이고 경구 활성인 이중 억제제입니다. SYN1143은 160~710nM 범위의 IC50으로 Lck, Tie2, Src 및 BTK에 대한 약한 억제 활성을 가지고 있습니다. SYN1143은 RON과 c-Met가 활성화되는 암 연구에 사용할 수 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 913376-84-8
Sample solution is provided at 25 µL, 10mM.
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SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC50s of 4 and 9 nM, respectively. SYN1143 has weak inhibitory activity on Lck, Tie2, Src, and BTK with IC50s ranging from 160 to 710 nM. SYN1143 can be used for the research of cancers that RON and c-Met are activated[1].
SYN1143 (Compound I) (10-1000 nM; 1 h) inhibits c-Met-mediated signaling and functional activity in HT-29 and BxPC3 cells[1].SYN1143 (10-1000 nM; 1 h) inhibits RON-mediated signaling and functional activity in NIH3T3 RON and BxPC3 cells[1].SYN1143 (0.3-30 μM; 2 h or 3 d) inhibits c-Met signaling and cell proliferation in MC3T3-E1 and C3H10T1/2 cells[2].SYN1143 (0.3-2 μM; 4-12 d) potentiates osteogenic differentiation of precursor cells[2].
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[1].SYN1143 (20-50 μg; transferred into calvarial defects) stimulates bone formation in critical-sized defects of mouse calvarial bone[2].
[1]. Zhang Y, et, al. Identification of a novel recepteur d’origine nantais/c-met small-molecule kinase inhibitor with antitumor activity in vivo. Cancer Res. 2008 Aug 15;68(16):6680-7.
[2]. Kim JW, et, al. Chemical inhibitors of c-Met receptor tyrosine kinase stimulate osteoblast differentiation and bone regeneration. Eur J Pharmacol. 2017 Jul 5;806:10-17.
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