NPS-1034
CAS号 | 1221713-92-3 | 货号 | BCP15998 |
中文名 | NPS-1034 | ||
英文名 | NPS-1034 | ||
中文别名 | |||
英文别名 | NPS1034;NPS 1034; | ||
分子式 | C31H23F2N5O3 | 分子量 | 551.54 |
生物活性 | NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.NPS-1034 is a novel MET inhibitor, which inhibits the activated MET receptor and its constitutively active mutants. NPS-1034, inhibits various constitutively active mutant forms of MET as well as HGF-activated wild-type MET. NPS-1034 inhibited the proliferation of cells expressing activated MET and promoted the regression of tumors formed from such cells in a mouse xenograft model through anti-angiogenic and pro-apoptotic actions. NPS-1034 also inhibited HGF-stimulated activation of MET signaling in the presence or absence of serum. Notably, NPS-1034 inhibited three MET variants that are resistant to the MET inhibitors SU11274, NVP-BVU972, and PHA665752. | ||
信号通路 | Angiogenesis/Protein Tyrosine Kinase | ||
靶 点 | TAM Receptor |
结构式
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