Crenolanib

Crenolanib is an orally bioavailable, selective inhibitor of type III tyrosine kinases with nanomolar potencies against platelet-derived growth factor receptor alpha (PDGFRalpha) and PDGFRbeta and Fms-related tyrosine kinase 3 (FLT3, IC50s = 11, 3.2, and 4 nM, respectively). It also inhibits medically-relevant mutant forms of these kinases, including the D842V-containing form of PDGFR and D835Y and internal tandem duplication mutations of FLT3, at nanomolar concentrations. Crenolanib is more than 100-fold selective for these kinases over other tyrosine and serine/threonine kinases. It is effective when used in cells and in vivo.Formal Name: 1-[2-[5-[(3-methyl-3-oxetanyl)methoxy]-1H-benzimidazol-1-yl]-8-quinolinyl]-4-piperidinamine. CAS Number: 670220-88-9. Synonyms: CP 868,596. Molecular Formula: C26H29N5O2. Formula Weight: 443.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 16 mg/ml, Ethanol: 10 mg/ml. lambdamax: 274 nm. SMILES: NC(CC1)CCN1C2=CC=CC3=C2N=C(N4C=NC5=C4C=CC(OCC6(C)COC6)=C5)C=C3. InChi Code: InChI=1S/C26H29N5O2/c1-26(14-32-15-26)16-33-20-6-7-22-21(13-20)28-17-31(22)24-8-5-18-3-2-4-23(25(18)29-24)30-11-9-19(27)10-12-30/h2-8,13,17,19H,9-12,14-16,27H2,1H3. InChi Key: DYNHJHQFHQTFTP-UHFFFAOYSA-N.