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Signaling Pathway

Crenolanib

HY-13223

(CP-868596; CP 868596; CP868596)

Crenolanib

Crenolanib Chemical Structure

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.

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $121 In-stock
5 mg $110 In-stock
10 mg $150 In-stock
50 mg $400 In-stock
100 mg $640 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €119 In-stock
5 mg €108 In-stock
10 mg €147 In-stock
50 mg €392 In-stock
100 mg €627 In-stock
200 mg Get quote
500 mg Get quote

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Product name: Crenolanib
Cat. No.: HY-13223

Crenolanib Data Sheet

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    Purity: 99.15%

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    DataSheet

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    COA

Related Compound Libraries

Biological Activity of Crenolanib

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) [1]
Target: 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 [1]. 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 [2].
in vivo:

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 443.54 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C26H29N5O2
CAS No 670220-88-9
Solvent & Solubility

DMSO ≥85mg/mL Water <1.2mg/mL Ethanol ≥6.6mg/mL

Preparing Stock Solutions

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

Clinical Information of Crenolanib

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

References on Crenolanib

Inhibitor Kit

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