Crenolanib, PDGFR and FLT3 inhibitor

Product Details

Formal Name: 1-[2-[5-[(3-Methyloxetan-3-yl)methoxy]benzimidazole-1-yl]quinoline-8-yl]piperidin-4-amine

Alternate Names: CP-868,596

Molecular Formula: C₂₆H₂₉N₅O₂

Formula Weight: 443.55

CAS Number: 670220-88-9

Purity: >97%

Formulation: powder

Solubility: Soluble in DMSO (up to 15 mg/ml) or in Ethanol (up to 10 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

PDGFR and FLT3 inhibitor

Functions

Crenolanib is a potent inhibitor of PDGFR (Kd for α = 2.1 nM; ß = 3.2 nM) and FLT3 (Kd = 0.74 nM). Crenolanib 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 I843 as well as FLT3/ITD and FLT3/D835 mutants.  Crenolanib acted synergistically with FLT3-CAR T-cells in a FLT3-ITD+ AML murine xenograft model.

Application Procedures

First dissolved in DMSO (up to 15 mg/ml) or in Ethanol (up to 10 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)