Biological Activity
(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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Chemical Information
Molecular Weight |
450.34 |
Formula |
C21H22Cl2FN5O |
CAS Number |
1374356-45-2 |
Purity |
>99% |
Solubility |
DMSO |
Storage |
at -20°C |