VRT752271

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)。

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库存: 现货

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价格

促销价

数量
5mg

￥987.00

790.00

- +
25mg

￥2825.00

2260.00

- +
100mg

￥5775.00

4620.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajci18304
CAS: 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
分子式: C21H22Cl2N4O2
分子量: 433.33
纯度: >98%
溶解度: ≥ 43.3mg/mL in DMSO
储存: Store at -20°C
库存: 现货

Background

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].

参考文献:
[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.