Synonym: BVD-523, Ulixertinib
In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib reduces the levels of phosphorylated ERK2 (pERK) and of the phosphorylation of the downstream kinase RSK (pRSK) with IC50 of 4.1/0.14 μM, respectively. Ulixertinib also inhibits A375 cell proliferation with IC50 of 180 nM.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||86 mg/mL in DMSO|
Determination of ulixertinib in mice plasma by LC-MS/MS and its application to a pharmacokinetic study in mice.
Kumar R, et al. J Pharm Biomed Anal. 2016 Jun 5;125:140-4. PMID: 27017572.
|Related ERK Products|
XMD8-92 is a potent and selective BMK1/ERK5 inhibitor with Kd of 80 nM.
DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM.
XMD17-109 is a novel, specific inhibitor of ERK-5 with an EC50 value of 4.2 μM in HEK293 cells.
GDC-0994 is a potent, orally available ERK inhibitor with IC50 1.1 nM and 0.3 nM, respectively.
FR 180204 is an ATP-competitive, selective ERK inhibitor with Ki of 0.31 μM and 0.14 μM for ERK1 And ERK2, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.