TSR-011-isomer
CAS No. : 1388225-79-3
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| Cat. No. : | HY-117806 |
| M.Wt: | 595.72 |
| Formula: | C33H43F2N5O3 |
| Purity: | >98 % |
| Solubility: |
TSR-011-isomer is an isomer of Belizatinib (HY-17603), a ALK inhibitor with an IC50 of 6 nM. TSR-011-isomer acts as a substrate for metabolic hydrolysis and NADPH-dependent metabolism. TSR-011-isomer undergoes enzymatic hydrolysis in mouse plasma and NADPH-dependent metabolism in mouse liver microsomes, thereby supporting clearance processes. TSR-011-isomer can be used in studies related to ALK-driven cancers[1].
In Vitro:TSR-011-isomer exhibits enhanced stability against mouse plasma-mediated hydrolysis, with a half-life of 2.9 h, an apparent plasma hydrolysis Vmax of 3.81 pmol/min·mL, and a Km of 0.357 μM[1].
TSR-011-isomer undergoes both hydrolysis and NADPH-dependent metabolism in mouse liver microsomes, with an apparent Vmax of 5.12 pmol/min·mg and a Km of 0.0292 μM for the hydrolysis reaction; the NADPH-dependent metabolism has a Vmax of 143 pmol/min·mg and a Km of 0.936 μM[1].
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