-crizotinib-chemical-structure.gif)
(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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[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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