TH287MTH1 inhibitor CAS# 1609960-30-6 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1609960-30-6 | SDF | Download SDF |
| PubChem ID | 73441664 | Appearance | Powder |
| Formula | C11H10Cl2N4 | M.Wt | 269.13 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 100 mg/mL (371.57 mM; Need ultrasonic) | ||
| Chemical Name | 6-(2,3-dichlorophenyl)-4-N-methylpyrimidine-2,4-diamine | ||
| SMILES | CNC1=NC(=NC(=C1)C2=C(C(=CC=C2)Cl)Cl)N | ||
| Standard InChIKey | URWCXPXBBITYLR-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C11H10Cl2N4/c1-15-9-5-8(16-11(14)17-9)6-3-2-4-7(12)10(6)13/h2-5H,1H3,(H3,14,15,16,17) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | TH287 is a potent inhibitor of MTH1 (NUDT1) with an IC50 value of 0.8 nM, less potent for MTH2, NUDT5, NUDT12, NUDT14, and NUDT16.
IC50 value: 0.8 nM [1]
Target: MTH1 inhibitor
TH287 is considered a new target for cancer therapy. TH287 is highly selective towards MTH1, with no relevant inhibition of other members of the nudix protein family. TH287 has been shown to selectively kill a variety of cancer cell lines, but is rapidly metablized, so not as useful for in vivo studies. References: | |||||
TH287 Dilution Calculator
TH287 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.7157 mL | 18.5784 mL | 37.1568 mL | 74.3135 mL | 92.8919 mL |
| 5 mM | 0.7431 mL | 3.7157 mL | 7.4314 mL | 14.8627 mL | 18.5784 mL |
| 10 mM | 0.3716 mL | 1.8578 mL | 3.7157 mL | 7.4314 mL | 9.2892 mL |
| 50 mM | 0.0743 mL | 0.3716 mL | 0.7431 mL | 1.4863 mL | 1.8578 mL |
| 100 mM | 0.0372 mL | 0.1858 mL | 0.3716 mL | 0.7431 mL | 0.9289 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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Development and validation of method for TH588 and TH287, potent MTH1 inhibitors and new anti-cancer agents, for pharmacokinetic studies in mice plasma.[Pubmed:25459754]
J Pharm Biomed Anal. 2015 Feb;104:1-11.
MTH1 is a protein that is required for cancer cell survival and is overexpressed in cancer cells. TH588 and TH287 are two new compounds that inhibit the MTH1 protein. The inhibitors were tested in pharmacokinetic studies on mice. A bioanalytical method was developed and validated for determination in mice plasma. The method was based on protein precipitation followed by LC-MS/MS analysis. The separation was performed on an Ascentis Express RP-Amide C18 column. The mass spectrometer was operated in positive electrospray ionization mode and the analytes were determined with multiple reaction monitoring (MRM). Abundant monoisotopic fragments were used for quantification. Two additional fragments were used for conformational analysis. The recovery of the compounds in plasma varied between 61 and 91% and the matrix effects were low and ranged between -3% and +2%. The method showed to be selective, linear, accurate and precise, and applicable for preclinical pharmacokinetic studies of TH588 and TH287 in mouse plasma. Half-life (T1/2) was
