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Technical Data
| Formula | C13H12Cl2N4 |
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| Molecular Weight | 295.17 | CAS No. | 1609960-31-7 | |
| Solubility (25°C)* | In vitro | DMSO | 20 mg/mL (67.75 mM) | |
| Ethanol | 2 mg/mL (6.77 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | TH588 is a potent and selective MTH1 (NUDT1) inhibitor with IC50 of 5 nM. It has no relevant inhibition of any of the other tested proteins at 100 μM, although TH588 showed reasonable selectivity when tested on a much larger panel of 87 enzymes, GPCRs, kinases, ion channels and transporters at 10 μM. | ||||
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| Targets |
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| In vitro | TH588 selectively kill U2OS and other cancer cell lines with less toxic to several primary or immortalized cells. TH588 also induces DNA damage and triggers an ATM-p53-mediated death response and DNA repair in U2OS cells. [1] | ||||
| In vivo | In mice bearing SW480 colorectal or MCF7 breast tumor xenografts, TH588 (30 mg/kg s.c.) reduces tumor growth via MTH1 inhibition. In mice carrying patient with BRAFV600E mutated xenografts, TH588 (30 mg/kg s.c.) also causes a reduced tumor growth rate. [1] |
Protocol (from reference)
| Animal Study: |
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Customer Product Validation
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Data from [Data independently produced by , , Anal Chim Acta, 2016, 905:66-71.]
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Data from [Data independently produced by , , Oncol Lett, 2018, 15(3):3240-3244]
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Data from [Data independently produced by , , Oncol Lett, 2017, 13(4):2161-2168]
Selleck's TH588 has been cited by 6 publications
| Platinum-based nanocomposites loaded with MTH1 inhibitor amplify oxidative damage for cancer therapy [ Colloids Surf B Biointerfaces, 2022, 218:112715] | PubMed: 35932557 |
| VISAGE Reveals a Targetable Mitotic Spindle Vulnerability in Cancer Cells. [ Cell Syst, 2019, 9(1):74-92.e8] | PubMed: 31302152 |
| TH588, an MTH1 inhibitor, enhances phenethyl isothiocyanate-induced growth inhibition in pancreatic cancer cells [Ikejiri F, et al. Oncol Lett, 2018, 15(3):3240-3244] | PubMed: 29435064 |
| Modification of tumour cell metabolism modulates sensitivity to Chk1 inhibitor-induced DNA damage. [Massey AJ Sci Rep, 2017, 7:40778] | PubMed: 28106079 |
| Expression and function of MutT homolog 1 in distinct subtypes of breast cancer. [Zhang X, et al. Oncol Lett, 2017, 13(4):2161-2168] | PubMed: 28454376 |
| Investigation of MTH1 activity via mismatch-based DNA chain elongation [Gao T, et al. Anal Chim Acta, 2016, 905:66-71] | PubMed: 26755138 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.