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
10 mM * 1 mL in DMSO USD 135 Get quote
5 mg USD 95 In-stock
Estimated Time of Arrival: December 31
10 mg USD 170 Get quote
25 mg USD 350 Get quote
50 mg USD 580 Get quote
100 mg USD 950 Get quote
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

4°C, stored under nitrogen, away from moisture

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

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

Purity: 99.42%

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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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