2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. VEGFR Dihydroorotate Dehydrogenase DNA/RNA Synthesis
  4. PTC299

PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies.

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

PTC299 Chemical Structure

PTC299 Chemical Structure

CAS No. : 1256565-36-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 319 In-stock
Solution
10 mM * 1 mL in DMSO USD 319 In-stock
Solid
1 mg USD 147 In-stock
5 mg USD 310 In-stock
10 mg USD 470 In-stock
50 mg USD 1400 In-stock
100 mg USD 2250 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

PTC299 Related Antibodies

Top Publications Citing Use of Products

View All VEGFR Isoform Specific Products:

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies[1][2].

IC50 & Target

VEGF[2]
Cellular Effect
Cell Line Type Value Description References
MOLM-13 CC50
6 nM
Compound: (S)-10e; 5, PTC299
Cytotoxicity against human MOLM-13 cells assessed as reduction of cell viability incubated for 3 days by CellTiter-Glo assay
Cytotoxicity against human MOLM-13 cells assessed as reduction of cell viability incubated for 3 days by CellTiter-Glo assay
[PMID: 36242990]
In Vitro

PTC299 inhibits hypoxia-induced VEGFA protein production in HeLa cells with an EC50 of 1.64 ± 0.83 nM[1].
PTC299 is the most potent inhibitor with an IC50 of about 1 nM, over 10 to 1000-fold more potent than Brequinar, Vidofludimus or A 77-1726 in leukemia cells[1].

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

PTC299 Related Antibodies
Clinical Trial
Molecular Weight

467.34

Formula

C25H20Cl2N2O3
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(N([C@H]1C2=CC=C(OC)C=C2)CCC3=C1NC4=C3C=C(Cl)C=C4)OC5=CC=C(Cl)C=C5
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 : 50 mg/mL (106.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1398 mL 10.6988 mL 21.3977 mL
5 mM 0.4280 mL 2.1398 mL 4.2795 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: ≥ 0.83 mg/mL (1.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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% Corn Oil

    Solubility: ≥ 0.83 mg/mL (1.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.89%

SDS (251 KB)

COA (253 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
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 2.1398 mL 10.6988 mL 21.3977 mL 53.4942 mL
5 mM 0.4280 mL 2.1398 mL 4.2795 mL 10.6988 mL
10 mM 0.2140 mL 1.0699 mL 2.1398 mL 5.3494 mL
15 mM 0.1427 mL 0.7133 mL 1.4265 mL 3.5663 mL
20 mM 0.1070 mL 0.5349 mL 1.0699 mL 2.6747 mL
25 mM 0.0856 mL 0.4280 mL 0.8559 mL 2.1398 mL
30 mM 0.0713 mL 0.3566 mL 0.7133 mL 1.7831 mL
40 mM 0.0535 mL 0.2675 mL 0.5349 mL 1.3374 mL
50 mM 0.0428 mL 0.2140 mL 0.4280 mL 1.0699 mL
60 mM 0.0357 mL 0.1783 mL 0.3566 mL 0.8916 mL
80 mM 0.0267 mL 0.1337 mL 0.2675 mL 0.6687 mL
100 mM 0.0214 mL 0.1070 mL 0.2140 mL 0.5349 mL
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PTC299 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:

PTC2991256565-36-2PTC 299PTC-299VEGFRDihydroorotate DehydrogenaseDNA/RNA SynthesisVascular endothelial growth factor receptorDHODHoraloff-targetkinasemyelosuppressionhematologicmalignanciescancerInhibitorinhibitorinhibit

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