ULIXERTINIB (BVD-523, VRT752271)

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.