Crenolanib
- CP-868596 - ARO-002 - Plarotinib
- Soluble in DMSO
- MF: C26H29N5O2
- MW: 443.54
Description
Crenolanib is an orally bioavailable, selective small molecule inhibitor of the Platelet-derived growth factor receptor (PDGFR) tyrosine kinase, inhibiting both purified PDGFRα and PDGFRβ with IC50s of 0.9 nM and 1.8 nM, respectively. It is also a type I pan-FLT3 inhibitor, highly selective over the closely related protein tyrosine kinase KIT, capable of inhibiting both FLT3/ITD and resistance-conferring FLT3/D835 mutants in vivo. It is considered to be an important next-generation FLT3 inhibitor.
More Information
| Parent CAS No. | 670220-88-9 |
|---|---|
| Chemical Name | 1-(2-(5-((3-Methyloxetan-3-yl)methoxy)-1H-benzo[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-amine |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C12C=CC(N3C=NC4C=C(OCC5(COC5)C)C=CC3=4)=NC=1C(N1CCC(N)CC1)=CC=C2 |
| MFCD | N.A. |
| InChi | 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 |
| InChiKey | DYNHJHQFHQTFTP-UHFFFAOYSA-N |
| CID | 10366136 |
| Short Description | PDGFRα, PDGFRβ and FLT3 inhibitor |
References
- MC Heinrich et al. Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors. Clin Cancer Res. 2012 Aug 15;18(16):4375-84.
- CC Smith et al. Crenolanib is a selective type I pan-FLT3 inhibitor. Proc Natl Acad Sci U S A. 2014 Apr 8;111(14):5319-24.
- A Galanis et al. Crenolanib is a potent inhibitor of FLT3 with activity against resistance-conferring point mutants. Blood. 2014 Jan 2;123(1):94-100.
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