Introduction：Basic information about CAS 252003-65-9|CP-547632, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | CP-547632 |
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| CAS Number | 252003-65-9 | Molecular Weight | 532.402 |
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| Density | 1.5±0.1 g/cm3 | Boiling Point | 548.6±50.0 °C at 760 mmHg |
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| Molecular Formula | C20H24BrF2N5O3S | Melting Point | / |
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| MSDS | / | Flash Point | 285.6±30.1 °C |
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Names
| Name | 3-[(4-bromo-2,6-difluorophenyl)methoxy]-5-(4-pyrrolidin-1-ylbutylcarbamoylamino)-1,2-thiazole-4-carboxamide |
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| Synonym | More Synonyms |
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CP-547632 BiologicalActivity
| Description | CP-547632 is a potent inhibitor of the VEGFR2 and FGF2 kinases with IC50s of 11 and 9 nM, respectively. |
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| Related Catalog | Signaling Pathways >>Protein Tyrosine Kinase/RTK >>VEGFRResearch Areas >>Cancer |
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| Target | IC50: 11 nM (VEGFR2), 9 nM (FGF2)[1] |
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| In Vitro | CP-547632 is an ATP-competitive kinase inhibitor that blocks VEGFR-2 kinase autophosphorylation (IC50=11 nM) and VEGF-induced VEGFR-2 phosphorylation in VEGFR-2-transfected endothelial cells (IC50=6 nM). CP-547632 is approximately equipotent (i.e., <10-fold selective) against VEGFR-2, bFGF receptor, and EGFR/Tie-2 chimera, the receptor for Angiopoietin[1]. |
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| In Vivo | CP-547632 inhibits tumor-associated VEGFR-2 phosphorylation resulting in decreased microvascular density and significant tumor growth inhibition in a number of tumor models (EC50=590 ng/mL). CP-547632 is shown to inhibit VEGF-induced angiogenesis in vivo in a dose-responsive fashion[1]. |
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| Cell Assay | Porcine aortic endothelial cells stably expressing full-length VEGFR-2 have been used. CP-547632 is added to serum-deprived cells and incubated at 37°C, 5% for 1 h. The cells are then stimulated with 500 ng/mL VEGF. Whole cell lysates are then immunoprecipitated using anti-VEGFR-2, and Western blot analysis is carried out with antibodies recognizing either the protein or PY (A) [1]. |
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| Animal Admin | Mice[1] MDA-MB-231 cells are injected s.c into the flank of BALB/c male mice. Animals bearing tumors of 75-150 mm3 each are treated with CP-547632 (6.25-100 mg/kg, p.o., qd) in 5% Gelucire. The tumors are measured with calipers, and the tumor volumes are calculated[1]. |
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| 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. |
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Chemical & Physical Properties
| Density | 1.5±0.1 g/cm3 |
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| Boiling Point | 548.6±50.0 °C at 760 mmHg |
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| Molecular Formula | C20H24BrF2N5O3S |
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| Molecular Weight | 532.402 |
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| Flash Point | 285.6±30.1 °C |
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| Exact Mass | 531.075134 |
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| PSA | 137.82000 |
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| LogP | 3.69 |
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| Vapour Pressure | 0.0±1.5 mmHg at 25°C |
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| Index of Refraction | 1.622 |
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| InChIKey | HXHAJRMTJXHJJZ-UHFFFAOYSA-N |
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| SMILES | NC(=O)c1c(OCc2c(F)cc(Br)cc2F)nsc1NC(=O)NCCCCN1CCCC1 |
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Safety Information
Customs
| HS Code | 2934999090 |
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| Summary | 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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Synonyms
| 3-(4-Bromo-phenoxymethyl)-benzoic acid |
| 3-(4-bromo-2,6-difluoro-benzyloxy)-5-[3-(4-pyrrolidin-1-yl-butyl)-ureido]-isothiazole-4-carboxylic acid amide |
| 3-(4-bromo-2,6-difluorobenzyloxy)-5-(3-(4-pyrrolidin-1-ylbutyl)ureido)isothiazole-4-carboxylic acid amide |
| 3-[(4-Bromo-2,6-difluorobenzyl)oxy]-5-({[4-(1-pyrrolidinyl)butyl]carbamoyl}amino)-1,2-thiazole-4-carboxamide |
| 3-[(4-bromo-2,6-difluorobenzyl)oxy]-5-({[4-(pyrrolidin-1-yl)butyl]carbamoyl}amino)-1,2-thiazole-4-carboxamide |
| 3-(4-Brom-benzyloxy)-benzoesaeure |
| 3-[(4-bromo-2,6-difluorophenyl)methoxy]-5-[[[[4-(1-pyrrolidinyl)butyl]amino]carbonyl]amino]-4-isothiazolecarboxamide |
| CP-547632 |
| 4-Isothiazolecarboxamide, 3-[(4-bromo-2,6-difluorophenyl)methoxy]-5-[[[[4-(1-pyrrolidinyl)butyl]amino]carbonyl]amino]- |
| 3-(4-bromo-benzyloxy)-benzoic acid |
