CP-547632
- Product Name
- CP-547632
- CAS No.
- 252003-65-9
- Chemical Name
- CP-547632
- Synonyms
- CS-1957;CP-547632;CP-547632(CP 547632);CP-547632 (PAN-90806);CP-547632, 10 mM in DMSO;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-carboxami;3-[(4-Bromo-2,6-difluorobenzyl)oxy]-5-[3-[4-(pyrrolidin-1-yl)butyl]ureido]isothiazole-4-carboxamide;3-(4-Bromo-2,6-difluorobenzyloxy)-5-(3-(4-pyrrolidin-1-ylbutyl)ureido)isothiazole-4-carboxylic acid amide;3-[(4-bromo-2,6-difluorophenyl)methoxy]-5-(4-pyrrolidin-1-ylbutylcarbamoylamino)-1,2-thiazole-4-carboxamide
- CBNumber
- CB82473822
- Molecular Formula
- C20H24BrF2N5O3S
- Formula Weight
- 532.4
- MOL File
- 252003-65-9.mol
CP-547632 Property
- 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
N-Bromosuccinimide Price
- Product number
- 21773
- Product name
- CP 547,632
- Purity
- ≥98%
- Packaging
- 500μg
- Price
- $57
- Updated
- 2024/03/01
- Product number
- 21773
- Product name
- CP 547,632
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $107
- Updated
- 2024/03/01
- Product number
- 21773
- Product name
- CP 547,632
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $437
- Updated
- 2024/03/01
- Product number
- CS-0003189
- Product name
- CP-547632
- Purity
- >99.0%
- Packaging
- 50mg
- Price
- $580
- Updated
- 2021/12/16
- Product number
- FB102944
- Product name
- 3-[(4-Bromo-2,6-difluorobenzyl)oxy]-5-[3-[4-(pyrrolidin-1-yl)butyl]ureido]isothiazole-4-carboxamide
- Packaging
- 25mg
- Price
- $750
- Updated
- 2021/12/16
CP-547632 Chemical Properties,Usage,Production
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
CP-547632 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from CP-547632 manufacturers
- Product
- CP-547632 252003-65-9
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- 95-99%
- Supply Ability
- 1ton
- Release date
- 2020-01-10