Crenolanib

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WARNING: This product is for research use only, not for human or veterinary use.

Description:Crenolanib is a n orally bioavailable small molecule, targeting the platelet-derived growth factor receptor (PDGFR), with potential antineoplastic activity. Crenolanib binds to and inhibits PDGFR, which may result in the inhibition of PDGFR-related signal transduction pathways, and, so, the inhibition of tumor angiogenesis and tumor cell proliferation.

Price and Availability

Crenolanib, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 205020Name: CrenolanibCAS#: 670220-88-9Chemical Formula: C26H29N5O2Exact Mass: 443.23213Molecular Weight: 443.54Elemental Analysis:C, 70.41; H, 6.59; N, 15.79; O, 7.21

Synonym:CP 868596; CP868596; CP-868596; ARO 002; RO-002; RO002; Crenolanib.

IUPAC/Chemical Name:1-(2-(5-((3-methyloxetan-3-yl)methoxy)-1H-benzo[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-amine.

InChi Key:DYNHJHQFHQTFTP-UHFFFAOYSA-N

InChi Code:InChI=1S/C26H29N5O2/c1-26(14-32-15-26)16-33-20-6-7-22-21(13-20)28-17-31(22)24-8-5-18-3-2-4-23(25(18)29-24)30-11-9-19(27)10-12-30/h2-8,13,17,19H,9-12,14-16,27H2,1H3

SMILES Code:NC1CCN(C2=C3N=C(N4C=NC5=CC(OCC6(C)COC6)=CC=C45)C=CC3=CC=C2)CC1

Technical Data

Additional Information

Crenolanib is an investigational new drug being developed by AROG Pharmaceuticals, LLC for the treatment of certain types of cancer. Crenolanib is a tyrosine kinase inhibitor that acts by specifically inhibiting the receptor tyrosine kinases PDGFRA and PDGFRB. Crenolanib is an orally bioavailable, selective small molecule inhibitor of the Platelet-derived growth factor receptor PDGFR) tyrosine kinase, inhibiting both PDGFRA and PDGFRB at picomolar concentrations.  Type III receptor tyrosine kinases (RTK), including c-KIT, PDGFRα and PDGFRβ, have been directly implicated in the pathogenesis of epithelial, mesenchymal, and hematological malignancies.[1] The PDGF/PDGFR pathway is the primary driver of oncogenesis in several malignancies including gastrointestinal stromal tumor (GIST),[2] both adult[3] and pediatric gliomas,[4] as well as a subset of Non-small-cell lung carcinoma (NSCLC).[5] These malignancies often respond to treatment with non-selective inhibitors of PDGFR like imatinib and sunitinib. Crenolanib is a 100-500-fold more potent inhibitor of PDGFRα and PDGFRβ than other commercially available TKIs. It is currently being developed as an antineoplastic agent in cancers. (source: http://en.wikipedia.org/wiki/ Crenolanib ).    

References

 1: Michael M, Vlahovic G, Khamly K, Pierce KJ,Guo F, Olszanski AJ. Phase Ib study of CP-868,596, a PDGFR inhibitor,combined with docetaxel with or without axitinib, a VEGFR inhibitor. BrJ Cancer. 2010 Nov 9;103(10):1554-61. Epub 2010 Oct 19. PubMed PMID:20959830; PubMed Central PMCID: PMC2990584.

2: Lewis NL, Lewis LD, Eder JP, Reddy NJ, Guo F, Pierce KJ, OlszanskiAJ, Cohen RB. Phase I study of the safety, tolerability, andpharmacokinetics of oral CP-868,596, a highly specific platelet-derivedgrowth factor receptor tyrosine kinase inhibitor in patients withadvanced cancers. J Clin Oncol. 2009 Nov 1;27(31):5262-9. Epub 2009 Sep8. PubMed PMID: 19738123; PubMed Central PMCID: PMC2773478.