TH287
Based on 3 publication(s) in Google Scholar
TH287 is a potent and selective inhibitor of MTH1, with an IC50 of 0.8 nM. TH287 is highly selective towards MTH1, with no relevant inhibition of MTH2, NUDT5, NUDT12, NUDT14, NUDT16, dCTPase, dUTPase and ITPA at 100 μM. TH287 could act as a chemotherapeutic agent for cancer research.
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- Purity : 98.99%
- CAS No.: 1609960-30-6
- 화학식: C11H10Cl2N4
- 분자량:269.13
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) TH287
MoreAll DNA/RNA Synthesis Isoforms
More
Biological Activity
제품 설명
IC50 & Target
IC50: 0.8 nM (MTH1)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MT4 | CC50 |
726 nM
Compound: TH287
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Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter glo assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter glo assay
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[PMID: 32184970] |
| SW480 | EC50 |
3 μM
Compound: TH287
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Cytotoxicity against human SW480 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter glo assay
Cytotoxicity against human SW480 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter glo assay
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[PMID: 32184970] |
| U2OS | EC50 |
0.7 μM
Compound: TH287
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Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by celltiter glo assay
Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by celltiter glo assay
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[PMID: 32184970] |
In Vitro
TH287 (1-10 μM; 24 h) selectively and effectively kills U2OS and other cancer cell lines, but is considerably less toxic to several primary or immortalized cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1609960-30-6
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Appearance Solid
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분자량 269.13
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화학식 C11H10Cl2N4
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Color White to off-white
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SMILES
NC1=NC(C2=CC=CC(Cl)=C2Cl)=CC(NC)=N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Sci Adv
A genetic screen for modifiers of cohesin clustering identifies regulators of genome folding. [Abstract]2026 Jan 30;12(5):eadx5130. PMID: 41616049 -
Acta Biomater
Delivery of MutT homolog 1 inhibitor by functionalized graphene oxide nanoparticles for enhanced chemo-photodynamic therapy triggers cell death in osteosarcoma. [Abstract]2020 Jun;109:229-243. PMID: 32294550 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471
용액&용해도
In Vitro:
DMSO : 100 mg/mL (371.57 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.29 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
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.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
순도&문서
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Data Sheet (277 KB)
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SDS (476 KB)
- English - EN (476 KB)
- Français - FR (476 KB)
- Deutsch - DE (476 KB)
- Norwegian - NO (476 KB)
- Español - ES (476 KB)
- Swedish - SV (476 KB)
- Italian - IT (476 KB)
- Korean - KR (476 KB)
- Portuguese - PT (476 KB)
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Handling Instructions (2659 KB)
References
[1]. Gad H, et al. MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool. Nature. 2014 Apr 10;508(7495):215-21. [Content Brief]
[2]. Saleh A, et, al. Development and validation of method for TH588 and TH287, potent MTH1 inhibitors and new anti-cancer agents, for pharmacokinetic studies in mice plasma. J Pharm Biomed Anal. 2015 Feb;104:1-11. [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 | 3.7157 mL | 18.5784 mL | 37.1568 mL | 92.8919 mL |
| 5 mM | 0.7431 mL | 3.7157 mL | 7.4314 mL | 18.5784 mL | |
| 10 mM | 0.3716 mL | 1.8578 mL | 3.7157 mL | 9.2892 mL | |
| 15 mM | 0.2477 mL | 1.2386 mL | 2.4771 mL | 6.1928 mL | |
| 20 mM | 0.1858 mL | 0.9289 mL | 1.8578 mL | 4.6446 mL | |
| 25 mM | 0.1486 mL | 0.7431 mL | 1.4863 mL | 3.7157 mL | |
| 30 mM | 0.1239 mL | 0.6193 mL | 1.2386 mL | 3.0964 mL | |
| 40 mM | 0.0929 mL | 0.4645 mL | 0.9289 mL | 2.3223 mL | |
| 50 mM | 0.0743 mL | 0.3716 mL | 0.7431 mL | 1.8578 mL | |
| 60 mM | 0.0619 mL | 0.3096 mL | 0.6193 mL | 1.5482 mL | |
| 80 mM | 0.0464 mL | 0.2322 mL | 0.4645 mL | 1.1611 mL | |
| 100 mM | 0.0372 mL | 0.1858 mL | 0.3716 mL | 0.9289 mL |
TH287 Related Classifications
HY-16965 Related Classifications
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