SYN1143 |
| カタログ番号GC62268 |
SYN1143 は、それぞれ 4 および 9 nM の IC50 を持つ、c-Met/RON の強力で選択的な経口活性二重阻害剤です。 SYN1143 は、Lck、Tie2、Src、および BTK に対して弱い阻害活性を持ち、IC50 は 160 ～ 710 nM の範囲です。 SYN1143は、RONやc-Metが活性化するがんの研究にご利用いただけます。
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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