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

CP-547632 TFA 

Cat. No.: HY-13302C Purity: 99.42%
Handling Instructions

CP-547632 TFA 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 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy.

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

CP-547632 TFA Chemical Structure

CP-547632 TFA Chemical Structure

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 135 In-stock
Estimated Time of Arrival: December 31
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 TFA 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 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy[1].

IC50 & Target[1]

VEGFR2

11 nM (IC50)

FGFR

9 nM (IC50)

In Vitro

CP-547632 TFA (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 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.
Molecular Weight

646.43

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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
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Keywords:

CP-547632CP547632CP 547632VEGFRFGFRVascular endothelial growth factor receptorFibroblast growth factor receptororallyATP-competitiveEGFRPDGFRβTKsantitumorVEGFR-2phosphorylationColo-205DLD-1MDA-MB-231Inhibitorinhibitorinhibit

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