TSR-011-isomer
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.
For research use only. We do not sell to patients.
- CAS No.: 1388225-79-3
- Formula: C33H43F2N5O3
- Molecular Weight:595.72
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Akt 6 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
536 nM
Compound: 49
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Inhibition of INSR expressed in CHO cells assessed as inhibition of receptor phosphorylation pre-incubated before insulin stimulation by Meso-Scale Discovery pY-IR assay
Inhibition of INSR expressed in CHO cells assessed as inhibition of receptor phosphorylation pre-incubated before insulin stimulation by Meso-Scale Discovery pY-IR assay
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[PMID: 22734674] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-inf | CL | MRT | T1/2 | Vss |
|---|---|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 0.957 μM·h | 3.51 L/h/kg | 1.28 h | 1.01 h | 4.49 L/kg |
Chemical Information
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CAS No. 1388225-79-3
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Molecular Weight 595.72
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Formula C33H43F2N5O3
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SMILES
O=C(C1=CC(F)=CC(F)=C1)/N=C2NC3=CC=C(C=C3N\2[C@H]4CC[C@H](CC4)C(NC(C)C)=O)CN5CCC(CC5)C(O)(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TSR-011-isomer Related Classifications
HY-117806 Related Classifications
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