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

CP-547632 TFA 

Cat. No.: HY-13302C Purity: 98.04%
COA 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
Solution
10 mM * 1 mL in DMSO USD 135 Ask For Quote & Lead Time
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 135 Ask For Quote & Lead Time
Solid
5 mg USD 95 Ask For Quote & Lead Time
10 mg USD 170 Ask For Quote & Lead Time
25 mg USD 350 Ask For Quote & Lead Time
50 mg USD 580 Ask For Quote & Lead Time
100 mg USD 950 Ask For Quote & Lead Time

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This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of CP-547632 TFA:

Other Forms of CP-547632 TFA:

Top Publications Citing Use of Products

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.
Clinical Trial
Molecular Weight

646.43

Appearance

Solid

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.
Purity & Documentation

Purity: 99.42%

COA (253 KB) HNMR (297 KB) LCMS (121 KB)

Handling Instructions (2659 KB)
References
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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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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

Keywords:

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

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