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Products are for research use only. Not for human use. We do not sell to patients.
(CP-868596; CP 868596; CP868596)
Crenolanib Chemical Structure
|Product name: Crenolanib|
|Cat. No.: HY-13223|
Crenolanib (CP-868596) is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src.
IC50 value: 2.1 nM/3.2 nM(PDGFRα/β) 
in vitro: 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 potent and selective PDGFR TKI. Crenolanib is a benzimidazole compound that has IC50s of 0.9 nM and 1.8 nM for PDGFRA and PDGFRB, respectively .
|M.Wt||443.54||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO ≥85mg/mL Water <1.2mg/mL Ethanol ≥6.6mg/mL
|1 mg||5 mg||10 mg|
|1 mM||2.2546 mL||11.2729 mL||22.5459 mL|
|5 mM||0.4509 mL||2.2546 mL||4.5092 mL|
|10 mM||0.2255 mL||1.1273 mL||2.2546 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|Crenolanib||Arog Pharmaceuticals||Acute myelogenous leukemia||31-JUL-12||30-APR-14||Phase 2||12-JUL-13|
|Pfizer Inc||Non-small-cell lung cancer||31-MAY-07||Phase 2||12-SEP-13|
|Arog Pharmaceuticals||Gastrointestinal stromal tumor||30-APR-11||30-SEP-14||Phase 2||14-SEP-13|
|Arog Pharmaceuticals||Glioma||30-APR-11||31-DEC-14||Phase 2||14-SEP-13|
|Arog Pharmaceuticals||Acute myelogenous leukemia||31-OCT-12||31-DEC-13||Phase 2||11-SEP-13|
. Heinrich M, et al. CP-868,596, a highly potent PDGFR inhibitor, inhibits phosphorylation of the imatinib-resistant PDGFRA D842V activating mutation associated with advanced GIST. AACR, 2011, Abstract 3586.
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