CP-547632
CP-547632 Basic information
- Product Name:
- CP-547632
- Synonyms:
-
- CP-547632
- 3-(4-Bromo-2,6-difluorobenzyloxy)-5-(3-(4-pyrrolidin-1-ylbutyl)ureido)isothiazole-4-carboxylic acid amide
- 4-Isothiazolecarboxamide, 3-((4-bromo-2,6-difluorophenyl)methoxy)-5-((((4-(1-pyrrolidinyl)butyl)amino)carbonyl)amino)-
- CP-547632(CP 547632)
- 3-[(4-broMo-2,6-difluorophenyl)Methoxy]-5-[[[[4-(1-pyrrolidinyl)butyl]aMino]carbonyl]aMino]-4-isothiazolecarboxaMide
- 3-((4-Bromo-2,6-difluorobenzyl)oxy)-5-(3-(4-(pyrrolidin-1-yl)butyl)ureido)isothiazole-4-carboxami
- 3-((4-Bromo-2,6-difluorobenzyl)oxy)-5-(3-(4-(pyrrolidin-1-yl)butyl)ureido)isothiazole-4-carbox
- 3-[(4-Bromo-2,6-difluorobenzyl)oxy]-5-[3-[4-(pyrrolidin-1-yl)butyl]ureido]isothiazole-4-carboxamide
- CAS:
- 252003-65-9
- MF:
- C20H24BrF2N5O3S
- MW:
- 532.4
- EINECS:
- 200-258-5
- Mol File:
- 252003-65-9.mol
CP-547632 Chemical Properties
- Boiling point:
- 548.6±50.0 °C(Predicted)
- Density
- 1.532
- storage temp.
- 2-8°C
- solubility
- DMSO: 94 mM
- form
- A solid
- pka
- 12.50±0.70(Predicted)
- color
- White to light yellow
- InChIKey
- HXHAJRMTJXHJJZ-UHFFFAOYSA-N
- SMILES
- S1C(NC(NCCCCN2CCCC2)=O)=C(C(N)=O)C(OCC2=C(F)C=C(Br)C=C2F)=N1
CP-547632 Usage And Synthesis
Description
CP 547,632 is an orally bioavailable and potent inhibitor of the receptor tyrosine kinases VEGF receptor 2 (VEGFR2) and basic fibroblast growth factor (bFGF) with IC50 values of 11 and 9 nM, respectively, in an enzyme assay. It is selective for VEGFR2 and bFGF over EGFR, PDGF receptor β (PDGFRβ), and related tyrosine kinases. CP 547,632 inhibits VEGFR2 autophosphorylation induced by VEGF in porcine aortic endothelial cells transfected with VEGFR2 (IC50 = 6 nM) and in a xenograft mouse model using NIH3T3/H-Ras cells (EC50 = 590 nM). It decreases angiogenesis induced by VEGF or bFGF and suppresses tumor growth in athymic mice.
Uses
CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy[1].
in vivo
CP-547632 (p.o.; 6.25-100 mg/kg/day; for 10-24 days) causes a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB-231 xenografts[1].
CP-547632 (oral; 50 mg/kg; a single oral dose) yieldes plasma concentrations above 500 ng/ml for 12 hours[1].
| Animal Model: | Athymic female mice (CD-1 nu/nu) bearing tumors (75-150 mm in size)[1] |
| Dosage: | 6.25, 12.5, 25, 50, 100 mg/kg |
| Administration: | PO; daily; 10-24 days |
| Result: | Caused a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB-231 xenografts. |
| Animal Model: | Female athymic mice bearing H-Ras tumor[1] |
| Dosage: | 50 mg/kg |
| Administration: | Oral |
| Result: | A single oral dose of 50 mg/kg yielded plasma concentrations above 500 ng/ml for 12 hours. |
IC 50
VEGFR-2: 11 nM (IC50); FGFR: 9 nM (IC50)
References
[1] Beebe JS, et al. Pharmacological characterization of CP-547,632, a novel vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for cancer therapy. Cancer Res. 2003 Nov 1;63(21):7301-9. PMID:14612527
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