PTC299
Based on 5 publication(s) in Google Scholar
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.71%
- CAS 番号: 1256565-36-2
- 分子式: C25H20Cl2N2O3
- 分子量:467.34
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
VEGF[2]
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Cell Line
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Type | Value | Description | References |
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| MOLM-13 | CC50 |
6 nM
Compound: (S)-10e; 5, PTC299
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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
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[PMID: 36242990] |
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1256565-36-2
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性状 Solid
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分子量 467.34
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分子式 C25H20Cl2N2O3
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Color White to light yellow
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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
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別名
Emvododstat
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Commun
DHODH modulates immune evasion of cancer cells via CDP-Choline dependent regulation of phospholipid metabolism and ferroptosis. [Abstract]2025 Apr 24;16(1):3867. PMID: 40274823 -
Mol Biol Rep
Study on the mechanism of heterogeneous tumor-associated macrophages in three subtypes of breast cancer through the integration of single-cell RNA sequencing and in vitro experiments. [Abstract]2024 Jun 1;51(1):720. PMID: 38824268 -
Am J Reprod Immunol
Salvianolic Acid B Promotes Placental and Decidual Angiogenesis by Restoring the Normal Expression of Hypoxia-Inducible Factor-1α/Vascular Endothelial Growth Factor in Mice With Recurrent Pregnancy Loss. [Abstract]2025 Jul;94(1):e70105. PMID: 40637198 -
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溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Cao L, et al. Targeting of Hematologic Malignancies with PTC299, A Novel Potent Inhibitor of DihydroorotateDehydrogenase with Favorable Pharmaceutical Properties. Mol Cancer Ther. 2019 Jan;18(1):3-16. [Content Brief]
[2]. Bender Ignacio RA, et al. Brief Report: A Phase 1b/Pharmacokinetic Trial of PTC299, a Novel PostTranscriptional VEGF Inhibitor, for AIDS-Related Kaposi's Sarcoma: AIDS Malignancy Consortium Trial 059. J Acquir Immune Defic Syndr. 2016 May 1;72(1):52-7. [Content Brief]
[3]. Packer RJ, et al. Phase I and pharmacokinetic trial of PTC299 in pediatric patients with refractory or recurrent central nervous system tumors: a PBTC study. J Neurooncol. 2015;121(1):217-224. [Content Brief]
[4]. Zeng Z, et al, Targeting dihydroorotate dehydrogenase in acute myeloid leukemia. Haematologica. 2018 Sep;103(9):1415-1417. [Content Brief]
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 |
PTC299 関連分類
HY-124593 関連分類
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