TRK-IN-33
TRK-IN-33 is a TRK inhibitor. TRK-IN-33 exhibits excellent TRKAG667C degradation (DC50 = 24.69 nM; Dmax > 90%), while sparing the wild-type protein in virto. TRK-IN-33 shows antiproliferative activities against Ba/F3-LMNA-NTRK1G667C cells with an IC50 value of 2.48 nM. TRK-IN-33 effectively inhibits tumor growth and enhances apoptosis in tumor tissues with no apparent toxicity in vivio. TRK-IN-33 can be used for NTRK fusion−positive cancers research.
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- Formule: C22H22ClFN6O3
- Masse moléculaire:472.90
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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TrkA |
TRK-IN-33 (compound 20) (0.1-10 μM) exhibits excellent degradation efficiency against TRKAG667C resistant mutation (degradation = -1.16% at 0.1 μM, degradation = 69.30% at 1 μM, degradation = 68.75% at 10 μM) and inhibitory activities with IC50 = 23.8 nM in Ba/F3-LMNA-NTRK1WT cells.[1].
TRK-IN-33 (0.1-10 μM, 24 h) displays favorable dose-dependent degradation on TRKA G667C mutant protein in Ba/F3-LMNA-NTRK1G667C cells[1].
TRK-IN-33 (1 μM) exhibits superior pharmacokinetic properties in CD-1 mice, SD rats, or humans microsomes with T1/2 = 24.8, 53.8 and 57.1min; CLint = 0.0683, 0.0599 and 0.0230 mL/min/mg, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3-LMNA-NTRK1G667C cells
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Concentration:0.1, 1 and 10 μM
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Incubation Time:24 h
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Result:Exhibited > 90% maximal degradation, potentially overcoming on-target resistance in TRKA G667C resistant mutation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Ba/F3-LMNA-NTRK1 sup>G667C cells (3 × 106) induced-female BALB/c nude mice (18-22 g, 4 weeks old)[1]
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Dosage:30 or 50 mg/kg
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Administration:i.p., twice daily for 28 consecutive days
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Result:Significantly inhibited tumor growth in a dose-dependent manner, with inhibition rates of 71.65 and 80.38% at 30 and 50 mg/kg, respectively.
Observed no statistically significant changes in body weight.
Revealed no apparent damage in major organs, including the heart, liver, spleen, lung, and kidney.
Revealed g a significant reduction of TRK fluorescence intensity.
Suppressed tumor cell proliferation and enhanced apoptosis in tumor tissues.
Chemical Information
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Masse moléculaire 472.90
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Formule C22H22ClFN6O3
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SMILES
FC1=C(NC(C2=NN(C(C)C)C(N)=C2C(N)=O)=O)C=C(NC(CC3=CC=C(Cl)C=C3)=O)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TRK-IN-33 Related Classifications
HY-180172 Related Classifications
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