Ulixertinib (BVD-523) | ERK1/2 inhibitor | Probechem Biochemicals

Chemical Structure : Ulixertinib

CAS No.: 869886-67-9

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Ulixertinib (BVD-523, VRT752271)

货号: PC-20222Not For Human Use, Lab Use Only.

BVD-523 (Ulixertinib) is a potent, selective, reversible, ATP-competitive ERK1/2 inhibitor with Ki of 0.3/0.04 nM, respectively.

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25 mg	￥2180	In stock
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生物&药学活性

BVD-523 (Ulixertinib) is a potent, selective, reversible, ATP-competitive ERK1/2 inhibitor with Ki of 0.3/0.04 nM, respectively.
BVD-523 demonstrated excellent ERK1/2 kinase selectivity based on biochemical counter-screens against 75 kinases.
BVD-523 inhibits cellular proliferation and enhances caspase-3/7 activity in vitro while demonstrating substrate inhibition despite increased ERK1/2 phorphorylation.
BVD-523 (25-100 mg/kg, PO, BID) demonstrates in vivo antitumor activity in BRAFV600E-mutant cancer cell line (A375 cell line) xenograft models, and dose-dependent antitumor activity in KRASG12C-mutant pancreatic cell line xenograft model, MIAPaCa2.
BVD-523 yielded synergistic antiproliferative effects in a BRAFV600E-mutant melanoma cell line xenograft model when used in combination with BRAF inhibition.

物理化学性质&存储条件

分子量	433.33
分子式	C21H22Cl2N4O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1H-Pyrrole-2-carboxamide, 4-[5-chloro-2-[(1-methylethyl)amino]-4-pyridinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-

参考文献

1. Germann UA, et al. Mol Cancer Ther. 2017 Nov;16(11):2351-2363.

Ulixertinib (BVD-523, VRT752271)

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物理化学性质&存储条件

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Ulixertinib (BVD-523, VRT752271)

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