VRT752271 free base · Synonyms: Ulixertinib | BVD-523

Ulixertinib is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases.

For research use only. Not for human or veterinary use.

Target ERK

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

VRT752271 structure

CAS No.: 869886-67-9

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
1 g	USD 485.00	BP-02323-1g	Inquire	Get quote
2 g	USD 776.00	BP-02323-2g	Inquire	Get quote
3 g	USD 931.00	BP-02323-3g	In stock	Get quote
5 g	USD 1,240.00	BP-02323-5g	Inquire	Get quote
10 g	USD 1,985.00	BP-02323-10g	In stock	Get quote

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Description

Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line.

Biological activity

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.

Identifiers

SMILES: CC(C)NC1=NC=C(Cl)C(=C1)C1=CNC(=C1)C(=O)N[C@H](CO)C1=CC=CC(Cl)=C1
InChIKey: KSERXGMCDHOLSS-LJQANCHMSA-N

Specifications

MW (average): 433.3310
Formula: C₂₁H₂₂Cl₂N₄O₂
CAS No.: 869886-67-9
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO, not in water

Documents

References

[1]. Ward RA, et al. Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. J Med Chem. 2015 Jun 11;58(11):4790-801.

[2]. Kumar R, et al. 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.

[3]. Changwen Ning, et al. Targeting ERK Enhances the Cytotoxic Effect of the Novel PI3K and mTOR Dual Inhibitor VS-5584 in Preclinical Models of Pancreatic Cancer. Oncotarget. 2017 Jul 4;8(27):44295-44311.

Same target

Search ERK

Same research area

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