Art. -Nr.: HY-13302

CP-547632

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

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.

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Reinheit: 99.94%
CAS. Nr.: 252003-65-9
Formel: C₂₀H₂₄BrF₂N₅O₃S
Molecular Weight:532.40

Speicherung:

4°C, stored under nitrogen

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

CP-547632 Chemical Structure

CAS. Nr.: 252003-65-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

VEGFR-2

11 nM (IC₅₀)

FGFR

9 nM (IC₅₀)

Alle VEGFR Isoform-spezifische Produkte anzeigen :

In Vitro

CP-547632 (1-1000 nM; 1 hours) inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion, with an IC₅₀ value of 6 nM^[1].

MedChemExpress (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 (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].

MedChemExpress (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 A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 252003-65-9
Appearance Solid
Molecular Weight 532.40
Formel C₂₀H₂₄BrF₂N₅O₃S
Color White to light yellow
SMILES

O=C(NC1=C(C(N)=O)C(OCC2=C(F)C=C(Br)C=C2F)=NS1)NCCCCN3CCCC3
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, stored under nitrogen

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

Publications (2)

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Journal Impact Factor

Cell Rep

VEGFR2 inhibition potentiates STING-mediated antitumor immunity. [Abstract]

2026 Jun 18;45(7):117576. PMID: 42313565
ACS Omega

Identification of New Modulators and Inhibitors of Palmitoyl-Protein Thioesterase 1 for CLN1 Batten Disease and Cancer. [Abstract]

2024 Feb 28;9(10):11870-11882. PMID: 38496939

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 115 mg/mL (216.00 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8783 mL

9.3914 mL

18.7829 mL

5 mM

0.3757 mL

1.8783 mL

3.7566 mL

10 mM

0.1878 mL

0.9391 mL

1.8783 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5.75 mg/mL (10.80 mM); Clear solution

This protocol yields a clear solution of ≥ 5.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (57.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8783 mL	9.3914 mL	18.7829 mL	46.9572 mL
	5 mM	0.3757 mL	1.8783 mL	3.7566 mL	9.3914 mL
	10 mM	0.1878 mL	0.9391 mL	1.8783 mL	4.6957 mL
	15 mM	0.1252 mL	0.6261 mL	1.2522 mL	3.1305 mL
	20 mM	0.0939 mL	0.4696 mL	0.9391 mL	2.3479 mL
	25 mM	0.0751 mL	0.3757 mL	0.7513 mL	1.8783 mL
	30 mM	0.0626 mL	0.3130 mL	0.6261 mL	1.5652 mL
	40 mM	0.0470 mL	0.2348 mL	0.4696 mL	1.1739 mL
	50 mM	0.0376 mL	0.1878 mL	0.3757 mL	0.9391 mL
	60 mM	0.0313 mL	0.1565 mL	0.3130 mL	0.7826 mL
	80 mM	0.0235 mL	0.1174 mL	0.2348 mL	0.5870 mL
	100 mM	0.0188 mL	0.0939 mL	0.1878 mL	0.4696 mL

CP-547632

2 Cited Publications

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CP-547632

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Publications Citing Use of MedChemExpress (MCE) CP-547632

Alle VEGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CP-547632 Related Classifications

HY-13302 Related Classifications