252003-65-9
252003-65-9 structure
- Name: CP-547632
- Chemical Name: 3-[(4-bromo-2,6-difluorophenyl)methoxy]-5-(4-pyrrolidin-1-ylbutylcarbamoylamino)-1,2-thiazole-4-carboxamide
- CAS Number: 252003-65-9
- Molecular Formula: C20H24BrF2N5O3S
- Molecular Weight: 532.402
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK VEGFR
- Create Date: 2018-12-28 05:39:48
- Modify Date: 2024-01-09 16:11:18
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CP-547632 is a potent inhibitor of the VEGFR2 and FGF2 kinases with IC50s of 11 and 9 nM, respectively.
| Name | 3-[(4-bromo-2,6-difluorophenyl)methoxy]-5-(4-pyrrolidin-1-ylbutylcarbamoylamino)-1,2-thiazole-4-carboxamide |
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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 |
| 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 | |
| Target |
IC50: 11 nM (VEGFR2), 9 nM (FGF2)[1] |
| 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]. |
| 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]. |
| 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]. |
| 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]. |
| References |
| Density | 1.5±0.1 g/cm3 |
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| Boiling Point | 548.6±50.0 °C at 760 mmHg |
| Molecular Formula | C20H24BrF2N5O3S |
| Molecular Weight | 532.402 |
| Flash Point | 285.6±30.1 °C |
| Exact Mass | 531.075134 |
| PSA | 137.82000 |
| LogP | 3.69 |
| Vapour Pressure | 0.0±1.5 mmHg at 25°C |
| Index of Refraction | 1.622 |
| HS Code | 2934999090 |
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| 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% |