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GDC-0994 1453848-26-4
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C21H18ClFN6O2 |
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439.85 |
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in stock | ||||
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1453848-26-4 |
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98%+ |
Introduction
GDC-0994 is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.
GDC-0994 (p.o.) results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice. [1] In vivo, GDC-0994 (p.o.) inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways, and subsequently prevents ERK-dependent tumor cell proliferation and survival. [2]