Crenolanib

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP02384CAS No. ：670220-88-9Purity：98%

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CAS No.	670220-88-9	Cat. No.	BCP02384
Name	Crenolanib
Synonyms	CP-868596;CP 868596;CP868596;ARO 002;
SMILES	NC1CCN(C2=CC=CC3=C2N=C(N4C5=CC=C(C=C5N=C4)OCC6(COC6)C)C=C3)CC1
Chemical Name
Formula	C26H29N5O2	M. Wt	443.54
Purity	98%	Storage	Store at 4-8°C
Description	Crenolanib is significantly more potent than imatinib in inhibiting the kinase activity of imatinib-resistant PDGFRα kinases (D842I, D842V, D842Y, D1842-843IM, and deletion I843). Crenolanib is 135-fold more otent than imatinib against D842V in the isogenic model system, with an IC50 of approximately 10 nM. Crenolanib inhibits the kinase activity of the fusion oncogene in EOL-1 cell line, which is derived from a patient with chronic eosinophilic leukemia and expresses the constitutively activated FIP1L1- PDGFRα fusion kinase, with IC50 = 21 nM. Crenolanib also inhibits the proliferation of EOL-1 cells with IC50 = 0.2 pM. Crenolanib inhibits the activation of V561D or D842V-mutant kinases expressed in BaF3 cells with IC50 with 85 nM or 272 nM, respectively. Crenolanib inhibits PDGFRα activation in H1703 non-small cell lung cancer cell line which has 24-fold amplification of the 4q12 region that contains the PDGFRα locus, with IC50 with 26 nM.Crenolanib is an orally bioavailable, highly