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(S)-crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition, induced an increase in DNA single-strand breaks, activated DNA repair in human colon carcinoma cells, and effectively suppressed tumour growth in animal models. Over all, (S)-crizotinib is an attractive chemical entity for further pre-clinical evaluation, and small-molecule inhibitors of MTH1 in general as a promising novel class of anticancer agents.
| Molecular Weight | 450.34 |
| Formula | C21H22Cl2FN5O |
| CAS Number | 1374356-45-2 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Alice T Shaw, et al. First-Line Lorlatinib or Crizotinib in Advanced ALK-Positive Lung Cancer
[2] D Ross Camidge, et al. Brigatinib versus Crizotinib in ALK-Positive Non-Small-Cell Lung Cancer
[4] Benjamin J Solomon, et al. First-line crizotinib versus chemotherapy in ALK-positive lung cancer
[5] Alice T Shaw, et al. Crizotinib in ROS1-rearranged non-small-cell lung cancer
| Related MTH1 Products |
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| TH588
TH588 is a first-in-class, potent, selective MTH1 (NUDT1) inhibitor with an IC50 value of 5 nM. |
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