TH287 |
| Catalog No.GC17601 |
TH287 es un inhibidor potente y selectivo de MTH1, con una IC50 de 0,8 nM. TH287 es altamente selectivo hacia MTH1, sin inhibiciÓn relevante de MTH2, NUDT5, NUDT12, NUDT14, NUDT16, dCTPase, dUTPase e ITPA a 100 μM. TH287 podrÍa actuar como agente quimioterapéutico para la investigaciÓn del cÁncer.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1609960-30-6
Sample solution is provided at 25 µL, 10mM.
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TH287 is a potent MTH1 inhibitor with IC50 of 0.8±0.1 nM. [1]
MTH1 (human MutT homolog 1) is an antimutagenic purine nucleoside triphosphatase that sanitize oxidized nucleotide pools. It’s a new cancer therapeutic target as it protects the cancer cell from DNA damages such as oxidative stress-induced cell dysfunction or death.
In U2OS and other cancer cell lines, TH287 treatment selectively and effectively kill cancer cells with less toxic to some primary or immortalized cells. U2OS cells treated with TH287 shows increase of 8-oxodG in DNA. The MTH1 inhibitor TH287 induces DNA damage and activates an ATM-p53-mediated death response and DNA repair in U2OS cells. [1]
Reference:
1. Gad H, Koolmeister T, Jemth AS et al. MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool. Nature. 2014 Apr 10;508(7495):215-21.
| Cas No. | 1609960-30-6 | SDF | |
| Chemical Name | 6-(2,3-dichlorophenyl)-N4-methylpyrimidine-2,4-diamine | ||
| Canonical SMILES | ClC1=C(Cl)C(C2=CC(NC)=NC(N)=N2)=CC=C1 | ||
| Formula | C11H10Cl2N4 | M.Wt | 269.13 |
| Solubility | ≥ 55.6mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7157 mL | 18.5784 mL | 37.1568 mL |
| 5 mM | 0.7431 mL | 3.7157 mL | 7.4314 mL |
| 10 mM | 0.3716 mL | 1.8578 mL | 3.7157 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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