1. Protein Tyrosine Kinase/RTK
  2. VEGFR FGFR
  3. CP-547632 hydrochloride

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.

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

CP-547632 hydrochloride Chemical Structure

CP-547632 hydrochloride Chemical Structure

CAS No. : 252003-71-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of CP-547632 hydrochloride:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE CP-547632 hydrochloride

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target[1]

VEGFR-2

11 nM (IC50)

FGFR

9 nM (IC50)

In Vitro

CP-547632 hydrochloride (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 hydrochloride (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 hydrochloride (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: Mice bearing tumors (75-150 mm in size)[1]
Dosage: 6.25, 12.5, 25, 50, 100 mg/kg
Administration: P.o.; daily; 10-24 days
Result: Caused a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB-231 xenografts.
Animal Model: H-ras tumor-bearing mice[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.
Molecular Weight

568.86

Formula

C20H25BrClF2N5O3S

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(NC1=C(C(N)=O)C(OCC2=C(F)C=C(Br)C=C2F)=NS1)NCCCCN3CCCC3.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (58.59 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7579 mL 8.7895 mL 17.5790 mL
5 mM 0.3516 mL 1.7579 mL 3.5158 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.88%

References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7579 mL 8.7895 mL 17.5790 mL 43.9475 mL
5 mM 0.3516 mL 1.7579 mL 3.5158 mL 8.7895 mL
10 mM 0.1758 mL 0.8790 mL 1.7579 mL 4.3948 mL
15 mM 0.1172 mL 0.5860 mL 1.1719 mL 2.9298 mL
20 mM 0.0879 mL 0.4395 mL 0.8790 mL 2.1974 mL
25 mM 0.0703 mL 0.3516 mL 0.7032 mL 1.7579 mL
30 mM 0.0586 mL 0.2930 mL 0.5860 mL 1.4649 mL
40 mM 0.0439 mL 0.2197 mL 0.4395 mL 1.0987 mL
50 mM 0.0352 mL 0.1758 mL 0.3516 mL 0.8790 mL
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CP-547632 hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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CP-547632 hydrochloride
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