Crenolanib (CP-868596) , 98% , 670220-88-9

CAS NO.：670220-88-9

Empirical Formula: C26H29N5O2

Molecular Weight: 443.54

MDL number: MFCD21609260

PRODUCT Properties

• Boiling point: 676.6±65.0 °C(Predicted)
• Density: 1.36
• storage temp.: -20°
• solubility: Soluble in DMSO (up to 15 mg/ml) or in Ethanol (up to 10 mg/ml).
• form: solid
• pka: 9.84±0.20(Predicted)
• color: White
• Stability: Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
• CAS DataBase Reference: 670220-88-9

Description and Uses

Crenolanib (670220-88-9) is a potent inhibitor of PDGFR (Kdfor α = 2.1 nM; β = 3.2 nM) and FLT3 (Kd= 0.74 nM).1Crenolanib is a type I inhibitor binding only to the active kinase conformation. It showed potent activity against imatinib-resistant PDGFRα mutations D842I, D842V, D842Y, DI842-843M, and deletion I8432as well as FLT3/ITD and FLT3/D835 mutants3. Crenolanib acted synergistically with FLT3-CAR T-cells in a FLT3-ITD+AML murine xenograft model.4

Crenolanib is an orally bioavailable, selective inhibitor of type III tyrosine kinases with nanomolar potencies against platelet-derived growth factor receptor α (PDGFRα) and PDGFRβ 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.[Cayman Chemical]

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H315-H319-H335
• Precautionary statements: P264-P280-P302+P352-P321-P332+P313-P362-P305+P351+P338-P337+P313-P261-P271-P304+P340-P312-P403+P233-P405-P501