MLN 2480

"目录号: HY-15246

MAPK/ERK Pathway-

MLN 2480 是一种可口服的，具有选择性的广谱的Raf抑制剂。

Raf

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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

NCT01425008

Millennium Pharmaceuticals, Inc.-Takeda

Melanoma-Metastatic Melanoma-Solid Tumor

September 15, 2011

Phase 1

NCT02327169

Millennium Pharmaceuticals, Inc.-Takeda

Advanced Nonhematologic Malignancies

February 2, 2015

Phase 1

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References

[1].Elizabeth Grace Carideo Cunniff, et al. Abstract C146: Combination treatment with the investigational RAF kinase inhibitor MLN2480 and the investigational MEK kinase inhibitor TAK-733 inhibits the growth of BRAF mutant and RAS mutant preclinical models of