BIX-02188

BIX-02188 is a potent inhibitor of MEK5 (IC50 = 4.3 nM) with reduced activity towards inhibition of ERK5 and TGFβR1 (IC50s = 810 and 1, 800 nM, respectively). Inhibition of MEK5 by BIX-02188 induces apoptosis in cells expressing the oncogenic mutant FLT3-ITD.

Product information

CAS Number: 334949-59-6

Molecular Weight: 412.48

Formula: C25H24N4O2

Chemical Name: (Z)-3-(((3-((dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxamide

Smiles: CN(C)CC1=CC(=CC=C1)N/C(=C1/C2=CC=C(C=C2NC/1=O)C(N)=O)/C1C=CC=CC=1

InChiKey: FSZPIAXLCCQFCM-FCQUAONHSA-N

InChi: InChI=1S/C25H24N4O2/c1-29(2)15-16-7-6-10-19(13-16)27-23(17-8-4-3-5-9-17)22-20-12-11-18(24(26)30)14-21(20)28-25(22)31/h3-14,27H,15H2,1-2H3,(H2,26,30)(H,28,31)/b23-22-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: ≥ 45 mg/mL

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

References:

1. Li L, et al. Fluid shear stress inhibits TNF-mediated JNK activation via MEK5-BMK1 in endothelial cells. Biochem Biophys Res Commun, 2008, 370(1), 159-163.
2. Tatake RJ, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun, 2008, 377(1), 120-125.

Products are for research use only. Not for human use.