Identification | Back Directory | [Name]
2H-Pyrido[3,2-b]-1,4-oxazine, 3,4-dihydro-2-[[6-[4-[2-(4-morpholinyl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-1,2,3-triazolo[4,5-b]pyrazin-1-yl]methyl]- | [CAS]
2079853-72-6 | [Synonyms]
2H-Pyrido[3,2-b]-1,4-oxazine, 3,4-dihydro-2-[[6-[4-[2-(4-morpholinyl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-1,2,3-triazolo[4,5-b]pyrazin-1-yl]methyl]- | [Molecular Formula]
C25H25F3N8O3 | [MOL File]
2079853-72-6.mol | [Molecular Weight]
542.51 |
Hazard Information | Back Directory | [Uses]
KRC-00715 is an effective oral c-Met inhibitor with an IC50 of 9.0 nM, demonstrating high selectivity in gastric cancer cells. KRC-00715 specifically inhibits the growth of c-Met-highly expressed cell lines by inducing G1/S phase arrest, leading to a reduction in downstream signaling pathways, including Akt and Erk, as well as c-Met activity. KRC-00715, in the gastric cancer cell line Hs746, is characterized by an IC50 of 39 nM, and it selectively inhibits the proliferation of c-Met-highly expressed cell lines. KRC-00715 reduces tumor size in Hs746T xenograft mouse models[1]. | [in vivo]
KRC-00715 (50 mg/kg; p.o.; once daily; 10 days) inhibited tumor volume increased in a nude mouse xenograft HS746T model[1]. Animal Model: | Nude mouse Hs746T xenograft model[1]. | Dosage: | 50 mg/kg | Administration: | oral gavage (p.o.);once daily; 10 days | Result: | Reduced the tumor volume, and the weight of mice did not reduce. |
| [References]
[1] Chi Hoon Park, et al. Novel c-Met inhibitor suppresses the growth of c-Met-addicted gastric cancer cells.BMC Cancer. 2016 Jan 22:16:35. DOI:10.1186/s12885-016-2058-y |
|
|