"目录号: HY-15246
MLN 2480 是一种可口服的，具有选择性的广谱的Raf抑制剂。
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生物活性
Description
MLN 2480 is an orally active and selective inhibitor ofpan-Rafkinase.
In Vitro
MLN2480 has effect on reversing feedback activation of MEK in response to TAK-733, leading to more concerted MAPK pathway inhibition[1].
In Vivo
MLN2480 inhibits MAPK pathway signaling in BRAF mutant and some RAS mutant preclinical cancer models at concentrations that are tolerated in vivo. MLN2480 is most potent in BRAF mutant melanoma models but also has single agent activity in some RAS mutant models. The combination of MLN2480 with TAK-733 inhibits the growth of a broader range of RAS mutant tumor models than single agent MLN2480, including primary human tumor xenograft models of melanoma and CRC[1]. ?
Clinical Trial
Millennium Pharmaceuticals, Inc.-Takeda
Melanoma-Metastatic Melanoma-Solid Tumor
September 15, 2011
Phase 1
Millennium Pharmaceuticals, Inc.-Takeda
Advanced Nonhematologic Malignancies
February 2, 2015
Phase 1
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References
