2. Protein Tyrosine Kinase/RTK
  3. PDGFR VEGFR
  4. TAK-593

TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.

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

TAK-593 Chemical Structure

TAK-593 Chemical Structure

CAS No. : 1005780-62-0

Size Price Stock Quantity
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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 143 In-stock
Solution
10 mM * 1 mL in DMSO USD 143 In-stock
Solid
5 mg USD 130 In-stock
10 mg USD 210 In-stock
25 mg USD 420 In-stock
50 mg USD 670 In-stock
100 mg USD 1050 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

TAK-593 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE TAK-593

View All PDGFR Isoform Specific Products:

View All Isoforms
PDGFR PDGFRβ PDGFRα

View All VEGFR Isoform Specific Products:

View All Isoforms
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.

IC50 & Target[1]

VEGFR1

3.2 nM (IC50)

VEGFR2

0.95 nM (IC50)

VEGFR3

1.1 nM (IC50)

PDGFRα

4.3 nM (IC50)

PDGFRβ

13 nM (IC50)

PDGFRαV561D

1 nM (IC50)

In Vitro

TAK-593 inhibits growth of HUVEC with an IC50 of 0.30 nM. It shows potent inhibitory activity against VEGFR (VEGFR1-3: IC50=3.2, 0.95, 1.1 nM) and PDGFR (PDGFRα, β: IC50=4.3, 13 nM) families. Against other kinases, the IC50 values of TAK-593 are above 100 nM, except for Fms (IC50=10 nM) and Ret (IC50=18 nM) kinases[1]. TAK-593 potently inhibits VEGF- and PDGF-stimulated cellular phosphorylation and proliferation of human umbilical vein endothelial cells and human coronary artery smooth muscle cells. TAK-593 also potently inhibits VEGF-induced tube formation of endothelial cells co-cultured with fibroblasts[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TAK-593 Related Antibodies
In Vivo

TAK-593 inhibits growth of HUVEC with an IC50 of 0.30 nM. It shows potent inhibitory activity against VEGFR (VEGFR1-3: IC50=3.2, 0.95, 1.1 nM) and PDGFR (PDGFRα, β: IC50=4.3, 13 nM) families. Against other kinases, the IC50 values of TAK-593 are above 100 nM, except for Fms (IC50=10 nM) and Ret (IC50=18 nM) kinases[1]. TAK-593 potently inhibits VEGF- and PDGF-stimulated cellular phosphorylation and proliferation of human umbilical vein endothelial cells and human coronary artery smooth muscle cells. TAK-593 also potently inhibits VEGF-induced tube formation of endothelial cells co-cultured with fibroblasts[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

445.47

Formula

C23H23N7O3
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=CC(C)=NN1C)NC2=CC(OC3=NN4C(C=C3)=NC(NC(C5CC5)=O)=C4)=CC=C2C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 48.5 mg/mL (108.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2448 mL 11.2241 mL 22.4482 mL
5 mM 0.4490 mL 2.2448 mL 4.4896 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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: ≥ 2.67 mg/mL (5.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 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: ≥ 2.67 mg/mL (5.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 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).
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: 99.66%

COA (246 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

Enzyme reactions are performed in 50 mM TrisHCl pH 7.5, 5 mM MnCl2, 5 mM MgCl2, 0.01% Tween-20 and 2 mM DTT, containing 10 μM ATP, 0.1 μg/mL biotinylated polyGluTyr (4:1) and 0.1 nM of VEGFR2. Prior to catalytic initiation with ATP, compound (TAK-593) and enzyme are incubated for 5 min at room temperature (preincubation). The reactions are quenched by the addition of 25 μL of 100 mM EDTA, 10 μg/mL AlphaScreen streptavidine donor beads and 10 μg/mL acceptor beads in 62.5 mM HEPES pH 7.4, 250 mM NaCl, and 0.1% BSA. Plates are incubated in the dark overnight and then read by plate reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

HUVECs are seeded into a 96-well plate at 3000 cells/well in Human Endothelial-SFM Growth Medium (Invitrogen) containing 3% fetal bovine serum (FBS) and are incubated overnight at 37 C in a 5% CO2 incubator. Various concentrations of the test compounds (TAK-593) are added in the presence of 60 ng/mL VEGF, and the cells are cultured for a further 5 days. Cellular proliferation is determined by the WST-8 formazan assay using Cell Counting Kit-8[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rats: The iv administration in rats is conducted under anesthesia with diethyl ether. At 5, 10 (only for iv dosing), 15, 30 min, and 1, 2, 3, 4, 6, 8, 12, 24, 32 (only for monkeys) and 48 h (only for monkeys) after dosing, blood is taken from the tail vein in rats or from the femoral vein in monkeys. Then, the blood is centrifuged to obtain the plasma fraction. The plasma is kept frozen at 20°C until analysis. The concentration of TAK-593 in plasma is determined by the high-performance liquid chromatography with a fluorescence detector. The excitation and emission are 346 and 420 nm, respectively.

Mice: Test compounds are administered at a dose of 10 mg/kg as a cassette dosing to nonfasted mice (BALB/cAJcl; female). After oral administration, blood samples are collected. The blood samples are centrifuged to obtain the plasma fraction. The plasma samples are deproteinized with acetonitrile containing an internal standard. After centrifugation, the supernatant is diluted with a mixture of 0.01 M ammonium formate solution and acetonitrile (9:1, v/v) and centrifuged again. The compound concentrations in the supernatant are measured by LC/MS/MS[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2448 mL 11.2241 mL 22.4482 mL 56.1205 mL
5 mM 0.4490 mL 2.2448 mL 4.4896 mL 11.2241 mL
10 mM 0.2245 mL 1.1224 mL 2.2448 mL 5.6121 mL
15 mM 0.1497 mL 0.7483 mL 1.4965 mL 3.7414 mL
20 mM 0.1122 mL 0.5612 mL 1.1224 mL 2.8060 mL
25 mM 0.0898 mL 0.4490 mL 0.8979 mL 2.2448 mL
30 mM 0.0748 mL 0.3741 mL 0.7483 mL 1.8707 mL
40 mM 0.0561 mL 0.2806 mL 0.5612 mL 1.4030 mL
50 mM 0.0449 mL 0.2245 mL 0.4490 mL 1.1224 mL
60 mM 0.0374 mL 0.1871 mL 0.3741 mL 0.9353 mL
80 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7015 mL
100 mM 0.0224 mL 0.1122 mL 0.2245 mL 0.5612 mL
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TAK-593 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.

Keywords:

TAK-5931005780-62-0TAK593TAK 593PDGFRVEGFRPlatelet-derived growth factor receptorVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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