CRENOLANIB
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| Catalog No. | APIM050132 |
|---|---|
| Product Name | CRENOLANIB |
Description
Background Information:
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 (Refs 2 & 3). It is considered to be an important next-generation FLT3 inhibitor.
Reference:
1. M. C Heinrich, et al., Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors. Clin Cancer Res, 2012, Jun 27.
2. C. C. Smith, et al, Crenolanib is a selective type I pan-FLT3 inhibitor, PNAS, April 8, 2014, Vol. 111, no. 14, 5319-5324.
3. A. Galanis, et al, Crenolanib is a potent inhibitor of FLT3 with activity against resistance-conferring point mutants, Blood , 11/2013; DOI: 10.1182/blood-2013-10-529313.
APIM050132: CRENOLANIB
CAS No.: 670220-88-9.
Molecular Formula: C26H29N5O2.
Molecular Weight: 443.54.
Purity: >99.5% (HPLC).
QC: HPLC-MS, 1HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO, and water with 1 eq. of acid.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
