VRT752271

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VRT752271

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

869886-67-9

包装与价格：

包装	价格(元)
5mg	电议
25mg	电议
100mg	电议

产品介绍

VRT752271 (BVD-523; VRT752271) 是一种有效的、具有口服活性、高度选择性、ATP 竞争性和可逆的 ERK1/2 激酶共价抑制剂，对 ERK2 的 IC50<0.3 nM。 VRT752271 (BVD-523; VRT752271) 抑制 A375 黑色素瘤细胞系中的磷酸化 ERK2 (pERK) 和下游激酶 RSK (pRSK)。

Cas No.	869886-67-9
别名	4-[5-氯-2-[(1-甲基乙基)氨基]-4-吡啶基]-N-[(1S)-1-(3-氯苯基)-2-羟基乙基]-1H-吡咯-2-甲酰胺,BVD-523; VRT752271
化学名	N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-4-[5-chloro-2-(propan-2-ylamino)pyridin-4-yl]-1H-pyrrole-2-carboxamide
Canonical SMILES	CC(C)NC1=NC=C(C(=C1)C2=CNC(=C2)C(=O)NC(CO)C3=CC(=CC=C3)Cl)Cl
分子式	C₂₁H₂₂Cl₂N₄O₂
分子量	433.33
溶解度	≥ 43.3mg/mL in DMSO
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	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[1][2]. 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[2]. 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.