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Chemical Structure : Ulixertinib
CAS No.: 869886-67-9
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $158 | In stock | |
| 25 mg | $248 | In stock | |
| 100 mg | $548 | In stock | |
| 1 g | Get quote |
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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.
| M.Wt | 433.33 | |
| Formula | C21H22Cl2N4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1H-Pyrrole-2-carboxamide, 4-[5-chloro-2-[(1-methylethyl)amino]-4-pyridinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]- |
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1. Germann UA, et al. Mol Cancer Ther. 2017 Nov;16(11):2351-2363.
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