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

CP-547632 

Cat. No.: HY-13302 Purity: 98.71%
Handling Instructions

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.

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

CP-547632 Chemical Structure

CP-547632 Chemical Structure

CAS No. : 252003-65-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 111 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 111 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 95 In-stock
Estimated Time of Arrival: December 31
10 mg USD 170 In-stock
Estimated Time of Arrival: December 31
25 mg USD 350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 580 In-stock
Estimated Time of Arrival: December 31
100 mg USD 950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target[1]

VEGFR-2

11 nM (IC50)

FGFR

9 nM (IC50)

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].

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].

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
Molecular Weight

532.40

Formula

C₂₀H₂₄BrF₂N₅O₃S

CAS No.
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 : 100 mg/mL (187.83 mM; Need ultrasonic)

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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 4 mg/mL (7.51 mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: 4 mg/mL (7.51 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 4 mg/mL (7.51 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: ≥99.0%

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