2. PI3K/Akt/mTOR Others Metabolic Enzyme/Protease
  3. Akt Drug Isomer NADPH Oxidase
  4. 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.

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TSR-011-isomer

TSR-011-isomer Chemical Structure

CAS No. : 1388225-79-3

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TSR-011-isomer Related Antibodies

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Akt Akt1 Akt2 Akt3

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NOX1 NOX2 NOX4 NOX5 DUOX1

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Description

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].

IC50 & Target[1]

Akt

6 nM (IC50)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TSR-011-isomer Related Antibodies
Parmacokinetics
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
Molecular Weight

595.72

Formula

C33H43F2N5O3
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TSR-011-isomer Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TSR-011-isomer1388225-79-3AktDrug IsomerNADPH OxidasePKBProtein kinase BNOXALK-expressing cellsNADPH-dependent metabolismalk-driven cancermouse plasmaenzymatic hydrolysismouse liver microsomesALKInhibitorinhibitorinhibit

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