Ulixertinib

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.

Product information

CAS Number: 869886-67-9

Molecular Weight: 433.33

Formula: C21H22Cl2N4O2

Synonym:

VRT752271

BVD-523

Chemical Name: (S)-4-(5-chloro-2-(isopropylamino)pyridin-4-yl)-N-(1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide.

Smiles: CC(C)NC1=CC(=C(Cl)C=N1)C1=CNC(=C1)C(=O)N[C@H](CO)C1=CC=CC(Cl)=C1

InChiKey: KSERXGMCDHOLSS-LJQANCHMSA-N

InChi: InChI=1S/C21H22Cl2N4O2/c1-12(2)26-20-8-16(17(23)10-25-20)14-7-18(24-9-14)21(29)27-19(11-28)13-4-3-5-15(22)6-13/h3-10,12,19,24,28H,11H2,1-2H3,(H,25,26)(H,27,29)/t19-/m1/s1

Technical Data

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

In Vitro:

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 Vivo:

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.

References:

1. 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.
2. 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.