1. Protein Tyrosine Kinase/RTK
  2. VEGFR

CP-547632 

Cat. No.: HY-13302
Handling Instructions

CP-547632 is a potent inhibitor of the VEGFR2 and FGF2 kinases with IC50s of 11 and 9 nM, respectively.

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

CP-547632 Chemical Structure

CP-547632 Chemical Structure

CAS No. : 252003-65-9

Size Stock
250 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

View All VEGFR Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

CP-547632 is a potent inhibitor of the VEGFR2 and FGF2 kinases with IC50s of 11 and 9 nM, respectively.

IC50 & Target

IC50: 11 nM (VEGFR2), 9 nM (FGF2)[1]

In Vitro

CP-547632 is an ATP-competitive kinase inhibitor that blocks VEGFR-2 kinase autophosphorylation (IC50=11 nM) and VEGF-induced VEGFR-2 phosphorylation in VEGFR-2-transfected endothelial cells (IC50=6 nM). CP-547632 is approximately equipotent (i.e., <10-fold selective) against VEGFR-2, bFGF receptor, and EGFR/Tie-2 chimera, the receptor for Angiopoietin[1].

In Vivo

CP-547632 inhibits tumor-associated VEGFR-2 phosphorylation resulting in decreased microvascular density and significant tumor growth inhibition in a number of tumor models (EC50=590 ng/mL). CP-547632 is shown to inhibit VEGF-induced angiogenesis in vivo in a dose-responsive fashion[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
References
Cell Assay

Porcine aortic endothelial cells stably expressing full-length VEGFR-2 have been used. CP-547632 is added to serum-deprived cells and incubated at 37°C, 5% for 1 h. The cells are then stimulated with 500 ng/mL VEGF. Whole cell lysates are then immunoprecipitated using anti-VEGFR-2, and Western blot analysis is carried out with antibodies recognizing either the protein or PY (A) [1].

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

Animal Administration
[1]

Mice[1]

MDA-MB-231 cells are injected s.c into the flank of BALB/c male mice. Animals bearing tumors of 75-150 mm3 each are treated with CP-547632 (6.25-100 mg/kg, p.o., qd) in 5% Gelucire. The tumors are measured with calipers, and the tumor volumes are calculated[1].

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

References
Molecular Weight

532.40

Formula

C₂₀H₂₄BrF₂N₅O₃S

CAS No.

252003-65-9

SMILES

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CP-547632
Cat. No.:
HY-13302
Quantity:

CP-547632

Cat. No.: HY-13302