[CAS NO. 2805804-54-8] CP-547632TFA

Name: CP-547632TFA
Brand: Arctom Scientific
SKU: HY-13302C

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PRODUCTS SPECIFICATIONS [2805804-54-8]

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Catalog

HY-13302C

Brand

MCE

CAS

2805804-54-8

DESCRIPTION [2805804-54-8]

Overview

MDL	-
Molecular Weight	646.43
Molecular Formula	C22H25BrF5N5O5S
SMILES	FC(F)(C(O)=O)F.O=C(NC1=C(C(N)=O)C(OCC2=C(F)C=C(Br)C=C2F)=NS1)NCCCCN3CCCC3

For research use only. We do not sell to patients.

Summary

CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC ₅₀ s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF over EGFR , PDGFRβ , and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy ^[1] .

IC50 & Target

VEGFR2

11 nM (IC ₅₀ )

FGFR

9 nM (IC ₅₀ )

In Vitro

CP-547632 TFA (1-1000 nM; 1 hours) inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion, with an IC ₅₀ value of 6 nM ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis ^[1]

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 TFA (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 TFA (oral; 50 mg/kg; a single oral dose) yieldes plasma concentrations above 500 ng/ml for 12 hours ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00074854	Pfizer	Lung Neoplasms	May 2002	Phase 1\|Phase 2
NCT00074867	Pfizer	Ovarian Neoplasms\|Peritoneal Neoplasms\|Fallopian Tube Neoplasms	October 2003	Phase 2
NCT00096239	Jonsson Comprehensive Cancer Center\|National Cancer Institute (NCI)	Fallopian Tube Cancer\|Ovarian Cancer\|Primary Peritoneal Cavity Cancer	December 2004	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 150 mg/mL ( 232.04 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5470 mL	7.7348 mL	15.4696 mL
5 mM	0.3094 mL	1.5470 mL	3.0939 mL
10 mM	0.1547 mL	0.7735 mL	1.5470 mL

* Please refer to the solubility information to select the appropriate solvent.

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.