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252003-71-7

252003-71-7 Structure

252003-71-7 Structure
IdentificationBack Directory
[Name]

CP-547632 (hydrochloride)
[CAS]

252003-71-7
[Synonyms]

CP-547632 HYDROCHLORIDE
CP-547632 hydrochloride >=98% (HPLC)
[Molecular Formula]

C20H25BrClF2N5O3S
[MDL Number]

MFCD20268381
[MOL File]

252003-71-7.mol
[Molecular Weight]

568.86
Chemical PropertiesBack Directory
[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
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H315-H319-H335
[Precautionary statements ]

P305+P351+P338
Hazard InformationBack Directory
[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.
< td class="col2"> H-ras tumor-bearing mice
Animal Model:
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 )

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