RO4987655

"目录号: HY-14719

MAPK/ERK Pathway-

RO4987655(CH-4987655)是口服活性的MAP2K1/MEK1抑制剂，IC50为5.2 nM，具有抗肿瘤活性。

MEK

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U0126-PD98059-Trametinib-Selumetinib-PD0325901-Cobimetinib-MEK162-Honokiol-CI-1040-OTS-964-Refametinib-AS703026-GDC-0623-BIX02189-Ro 5126766-

生物活性

Description

RO4987655(CH-4987655) is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1/MEK1 IC50=5.2 nM), with potential antineoplastic activity.IC50 value: 5.2 nMTarget: MEK1/2MEK inhibitor RO4987655 binds to and inhibits MEK, which may result in the inhibition of MEK-dependent cell signaling and the inhibition of tumor cell proliferation. MEK, a dual specificity threonine/tyrosine kinase, is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers.

Clinical Trial

NCT00817518

Hoffmann-La Roche

Neoplasms

January 2009

Phase 1

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References

[1].Lee L, et al. The safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of CH4987655 in healthy volunteers: target suppression using a biomarker. Clin Cancer Res. 2009 Dec 1;15(23):7368-74.

[2].Leijen S, et al. Phase I dose-escalation study of the safety, pharmacokinetics, and pharmacodynamics of the MEK inhibitor RO4987655 (CH4987655) in patients with advanced solid tumors. Clin Cancer Res. 2012 Sep 1;18(17):4794-805.

[3].Kraeber-Bodéré F, et al. Differences in the biologic activity of 2 novel MEK inhibitors revealed by 18F-FDG PET: analysis of imaging data from 2 phase I trials. J Nucl Med. 2012 Dec;53(12):1836-46.