Ulixertinib (BVD-523, VRT752271)是一种高效、口服、高选择性的ERK1/2可逆共价抑制剂。它通过ATP竞争方式发挥作用,并能有效抑制ERK2及其下游蛋白RSK的磷酸化。
|
英文别名 (English Synonym) |
VRT752271 |
|
中文名称 (Chinese Name) |
|
|
靶点 (Target) |
ERK |
|
通路 (Pathway) |
MAPK/ERK |
|
CAS号 (CAS NO.) |
869886-67-9 |
|
分子式 (Formula) |
C21H22Cl2N4O2 |
|
分子量 (Molecular Weight) |
433.33 |
|
纯度 (Purity) |
≥98% |
|
溶解性 (Solubility) |
溶于DMSO |
-25~-15℃保存，有效期3年
[1] Ning C, Liang M, Liu S, Wang G, Edwards H, Xia Y, Polin L, Dyson G, Taub JW, Mohammad RM, Azmi AS, Zhao L, Ge Y. 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. doi: 10.18632/oncotarget.17869. PMID: 28574828, PMCID: PMC5546481.[2]Kumar R, Suresh PS, Rudresh G, Zainuddin M, Dewang P, Kethiri RR, Rajagopal S, Mullangi R. 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. doi: 10.1016/j.jpba.2016.03.036. Epub 2016 Mar 17. PMID: 27017572.
