Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
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||
10 mM in DMSO
|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.
Amuvatinib (MP-470) is a potent and multi-targeted inhibitor of c-Kit, PDGFR(alpha) and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively.
Axitinib(AG013736) blocked phosphorylation of VEGFR-2 and VEGFR-3 with average IC50s of 0.2 and 0.1 to 0.3 nM.
AZD2932 is a new series of quinazoline ether inhibitor which potently inhibits VEGFR-2 and PDGFR with IC50s of 4 nM/8 nM/ 7 nM for PDGFR(beta)/VEGFR-2/Flt-3.
BIBF 1202 is the carboxylate metabolite of BIBF 1120, which is an oral triple angiokinase inhibitor targeting VEGFR, PDGFR, FGFR.
CP 673451 is a selective inhibitor of PDGFR(alpha)/(beta) with IC50 of 10 nM/1 nM, exhibits >450-fold selectivity over other angiogenic receptors, has antiangiogenic and antitumor activity.
JI-101 is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor (beta) (PDGFR-(beta)), and ephrin type-B receptor 4 (EphB4). JI-101 inhibits angiogenesis, and subsequently tumor growth. 
Linifanib (ABT-869; AL-39324) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFR(beta) with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively.
N-desethyl sunitinib(SU-11662) is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFR(beta) and KIT inhibitor (Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFR(beta) and KIT respectively).
Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFR(alpha), VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively.
PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.