2. Neuronal Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. Trk Receptor Apoptosis
  4. 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.

For research use only. We do not sell to patients.

TRK-IN-33

TRK-IN-33 Chemical Structure

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TRK-IN-33 Related Antibodies

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Description

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[1].

IC50 & Target[1]

TrkA

 

In Vitro

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.

TRK-IN-33 Related Antibodies

Cell Viability Assay[1]

Cell Line: Ba/F3-LMNA-NTRK1G667C cells
Concentration: 0.1, 1 and 10 μM
Incubation Time: 24 h
Result: Exhibited > 90% maximal degradation, potentially overcoming on-target resistance in TRKA G667C resistant mutation.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ CL MRT0-t MRT0-∞ F
Mice[1] 1 mg/kg i.v. 0.249 h 0.083 h 590 ng/mL 231 ng·h/mL 232 ng·h/mL 442 mL/h/kg 0.268 h 0.275 h /
Mice[1] 10 mg/kg p.o. 0.437 h 0.500 h 754 ng/mL 930 ng·h/mL 932 ng·h/mL 4313 mL/h/kg 0.903 h 0.911 h 40.2 %
In Vivo

TRK-IN-33 (compound 20) (30 or 50 mg.kg, i.p., twice daily for 28 consecutive days) overcomes TRK resistance driven by the G667C mutation with good tolerability and safety profile in the Ba/F3-LMNA-NTRK1G667C mice xenograft model[1].

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

Animal Model: Ba/F3-LMNA-NTRK1 sup>G667C cells (3 × 106) induced-female BALB/c nude mice (18-22 g, 4 weeks old)[1]
Dosage: 30 or 50 mg/kg
Administration: i.p., twice daily for 28 consecutive days
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.
Molecular Weight

472.90

Formula

C22H22ClFN6O3
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
Shipping

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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TRK-IN-33 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:

TRK-IN-33Trk ReceptorApoptosisTropomyosin related kinase receptor TRKA G667C degradationinhibits tumor growthNTRK fusion?positive cancersTRKInhibitorinhibitorinhibit

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