CP-547632 (hydrochloride)
- Product Name
- CP-547632 (hydrochloride)
- CAS No.
- 252003-71-7
- Chemical Name
- CP-547632 (hydrochloride)
- Synonyms
- CP-547632 HYDROCHLORIDE;CP-547632 hydrochloride【PZ0264】;CP-547632 hydrochloride (PAN-90806);CP-547632 hydrochloride >=98% (HPLC);CP 547632 hydrochloride,CP547632 hydrochloride
- CBNumber
- CB52671229
- Molecular Formula
- C20H25BrClF2N5O3S
- Formula Weight
- 568.86
- MOL File
- 252003-71-7.mol
CP-547632 (hydrochloride) Property
- storage temp.
- Store at -20°C
- solubility
- DMSO: 38.33 mg/mL (67.38 mM); Water: < 0.1 mg/mL (insoluble)
- form
- Solid
- color
- White to light yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0025143
- Product name
- CP-547632(hydrochloride)
- Purity
- 98.24%
- Packaging
- 5mg
- Price
- $95
- Updated
- 2021/12/16
- Product number
- CS-0025143
- Product name
- CP-547632(hydrochloride)
- Purity
- 98.24%
- Packaging
- 10mg
- Price
- $170
- Updated
- 2021/12/16
- Product number
- CS-0025143
- Product name
- CP-547632(hydrochloride)
- Purity
- 98.24%
- Packaging
- 25mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0025143
- Product name
- CP-547632(hydrochloride)
- Purity
- 98.24%
- Packaging
- 50mg
- Price
- $580
- Updated
- 2021/12/16
- Product number
- CS-0025143
- Product name
- CP-547632(hydrochloride)
- Purity
- 98.24%
- Packaging
- 100mg
- Price
- $950
- Updated
- 2021/12/16
CP-547632 (hydrochloride) Chemical Properties,Usage,Production
Uses
CP-547632 hydrochloride 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 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy[1].
Biological Activity
CP-547632 hydrochloride is an orally active, ATP-competitive VEGFR-2 and FGF kinase inhibitor with IC50 of 11 nM and 9 nM, respectively. It is selective for VEGFR2 and bFGF over EGFR, PDGFRβ and related tyrosine kinases (TKs), and has an antitumor effects.
in vitro
CP-547632 hydrochloride (1-1000 nM; 1 hour) inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion, with an IC 50 value of 6 nM.
Western Blot Analysis
| Cell Line: | Serum-deprived cells |
| Concentration: | 1, 4, 16, 63, 250, 1000 nM |
| Incubation Time: | 1 hours |
| Result: | Inhibited VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion. |
in vivo
CP-547632 hydrochloride (po; 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.
CP-547632 hydrochloride (oral; 50 mg/kg; a single oral dose) yieldes plasma concentrations above 500 ng/ml for 12 hours.
| Animal Model: | Mice bearing tumors (75-150 mm in size) |
| 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: | < td class="col2"> H-ras tumor-bearing mice|
| 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. |
target
| VEGFR-2 < span> 11 nM (IC 50 ) | FGFR 9 nM (IC 50 ) |
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 (hydrochloride) Preparation Products And Raw materials
Raw materials
Preparation Products
CP-547632 (hydrochloride) Suppliers
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