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Background Information:
Ulixertinib (BVD-523, VRT752271) is a cell permeable small-molecule ERK1/2 kinase inhibitor currently under clinical investigation (Phase 1). It potently and selectively inhibits ERK1 and ERK2 kinases in a reversible, ATP-competitive fashion. Inhibits signal transduction, cell proliferation, and cell survival, most potently in cell lines bearing mutations that activate MAPK pathway signaling. Single-agent Ulixertinib inhibits tumor growth in vivo in BRAF-mutant melanoma and colorectal xenografts as well as in KRAS-mutant colorectal and pancreatic models. Combination treatment with Ulixertinib and Dabrafenib inhibits tumor growth in a BRAF-mutant melanoma model.
Reference:
1. The monohydrochloride salt, a clinical Formulation Format, is confirmed by a spot-on high-precision quantitative elemental analysis.
APIM050250: ULIXERTINIB (BVD-523, VRT752271)
CAS No.: 869886-67-9.
Molecular Formula: C21H22Cl2N4O2 ? HCl.
Molecular Weight: 469.8.
Purity: 100% optical purity (Chiral HPLC), 99.5% chemical purity (HPLC at 214 and 254 nm).
QC: HPLC-MS, 1HNMR, Chiral HPLC and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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