For research use only. Not for therapeutic Use.
CP-547632 (Cat.No:I006230), also known as PAN-90806, is as a potent inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases (IC50 11 and 9 nM, respectively). It is selective relative to epidermal growth factor receptor, platelet-derived growth factor , and other related TKs. It also inhibits VEGF-stimulated autophosphorylation of VEGFR-2 in a whole cell assay with an IC50 value of 6 nM. After oral administration of CP-547,632 to mice bearing NIH3T3/H-ras tumors, VEGFR-2 phosphorylation in tumors was inhibited in a dose-dependent fashion (EC50 590 ng/ml). CP-547,632 is a well-tolerated, orally-bioavailable inhibitor presently under clinical investigation for the treatment of human malignancies.
| Catalog Number | I006230 |
| CAS Number | 252003-65-9 |
| Synonyms | CP547632; CP 547632; CP-547632; PAN90806; PAN 90806; PAN-90806; CP632; OSI632; CP 632; OSI 632; CP-632; OSI-632;3-(4-bromo-2,6-difluorobenzyloxy)-5-(3-(4-(pyrrolidin-1-yl)butyl)ureido)isothiazole-4-carboxamide |
| Molecular Formula | C20H24BrF2N5O3S |
| Purity | ≥95% |
| Solubility | Soluble in DMSO, not in water |
| Storage | Store at -20°C |
| IC50 | IC50 = 9 Nm |
| IUPAC Name | 3-[(4-bromo-2,6-difluorophenyl)methoxy]-5-(4-pyrrolidin-1-ylbutylcarbamoylamino)-1,2-thiazole-4-carboxamide |
| InChI | InChI=1S/C20H24BrF2N5O3S/c21-12-9-14(22)13(15(23)10-12)11-31-18-16(17(24)29)19(32-27-18)26-20(30)25-5-1-2-6-28-7-3-4-8-28/h9-10H,1-8,11H2,(H2,24,29)(H2,25,26,30) |
| InChIKey | HXHAJRMTJXHJJZ-UHFFFAOYSA-N |
| SMILES | C1CCN(C1)CCCCNC(=O)NC2=C(C(=NS2)OCC3=C(C=C(C=C3F)Br)F)C(=O)N |
| Reference | </br>1:Cohen RB, Langer CJ, Simon GR, Eisenberg PD, Hainsworth JD, Madajewicz S, Cosgriff TM, Pierce K, Xu H, Liau K, Healey D. A phase I/randomized phase II, non-comparative, multicenter, open label trial of CP-547,632 in combination with paclitaxel and carboplatin or paclitaxel and carboplatin alone as first-line treatment for advanced non-small cell lung cancer (NSCLC). Cancer Chemother Pharmacol. 2007 Jun;60(1):81-9. Epub 2006 Oct 10. PubMed PMID: 17031646. |
