Ulixertinib, also known as BVD-523 and VRT752271, is an inhibitors of ERK protein kinase. Downmodulation of ERK protein kinase activity inhibits VEGF secretion by human myeloma cells and myeloma-induced angiogenesis. Upon oral administration, BVD-523 inhibits both ERK 1 and 2, thereby preventing the activation of ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is often upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival.
CAS Number: 869886-67-9
Molecular Weight: 433.33
Chemical Name: (S)-4-(5-chloro-2-(isopropylamino)pyridin-4-yl)-N-(1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide.
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
Combined Ulixertinib (BVD-523; 10, 20, 30 μM; 48 hours) and VS-5584 treatment causes significant induction of cell death in human pancreatic cancer (HPAC) cells in PDAC cell lines BxPC-3, MIAPaCa-2, and CFPAC-1.
In the pharmacokinetic study, the sensitivity and specificity of the assay are found to be sufficient for accurately characterizing the plasma pharmacokinetics of Ulixertinib (VRT752271) in Balb/C mice.
- Kumar R, Suresh PS, Rudresh G, Zainuddin M, Dewang P, Kethiri RR, Rajagopal S, Mullangi R. Determination of ulixertinib in mice plasma by LC-MS/MS and its application to a pharmacokinetic study in mice. J Pharm Biomed Anal. 2016 Jun 5;125:140-4. doi: 10.1016/j.jpba.2016.03.036. PubMed PMID: 27017572.
- Martinez-Botella; Gabriel (West Roxbury, MA), Hale; Michael (Bedford, MA), Maltais; Francois (Tewksbury, MA), Straub; Judith (Santa Cruz, CA), Tang; Qing (Acton, MA), Pyrrole inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto, US7,354,939 (2008).
Products are for research use only. Not for human use.
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