TRK-IN-32
TRK-IN-32 is a potent TRK inhibitor. TRK-IN-32 potently inhibits TRKWT, TRKG595R and TRKG667C with IC50 values of 0.08 nM, 2.14 nM and 0.68 nM, respectively. TRK-IN-32 also demonstrates antiproliferative activity against a panel of Ba/F3 cell lines transformed with wild type, xDFG, solvent-front as well as gatekeeper mutant TRK fusion proteins. TRK-IN-32 induces apoptosis of Ba/F3-TRKAWT and Ba/F3-TRKAG667C cells.TRK-IN-32 can be used for the study of various cancers (such as thyroid cancer, secretory breast carcinoma).
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- CAS No.: 3044124-79-7
- 화학식: C19H18FN7
- 분자량:363.39
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
TRK-IN-32 (Compound 15m) exhibits moderate human liver microsomal stability (t1/2 = 33.8 min)[1].
TRK-IN-32 exhibits anti-proliferative efficacy against Ba/F3 cell lines, with an IC50s of 1.24 (Ba/F3-ETV6-TRKAWT), 0.35 (Ba/F3-ETV6-TRKBWT), 24.26 (Ba/F3-LMNA-TRKAG595R), 10.24 (Ba/F3-LMNA-TRKAG667C) and 1.06 (Ba/F3-LMNA-TRKAF589L) nM[1].
TRK-IN-32 (0-10 nM) effectively blocks the TRKAWT and TRKAG667C autophosphorylation in cells at relatively low concentrations as well as phosphorylation of their downstream molecules AKT, PLCγ1 and ERK in Ba/F3 cells expressing TRKAWT and TRKAG667C fusion mutant[1].
TRK-IN-32 (0-500 nM, 48 h) strongly induces Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKAG667C cells apoptosis[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-CD74-TRKA and Ba/F3-CD74-TRKAG667C cells
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Concentration:10, 50, 100, 500 nM
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Incubation Time:48 h
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Result:Observed significant apoptosis rates of 18.74% at 100 nM and 35.65% at 500 nM in Ba/F3-CD74-TRKA cells.
Induced noticeable apoptosis rates of 11.22% and 56.25%, respectively. at concentrations of 10 nM and 50 nM in Ba/F3-CD74-TRKAG667C cells.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-inf | Vd | CL | MRT0-t | MRT0-inf | F |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | p.o. | 2.43 h | 2.00 h | 1363.33 ng/mL | 5581.58 ng·h/mL | 5582.96 ng·h/mL | 6454.96 mL/kg | 1810.18 mL/h/kg | 2.77 h | 2.78 h | 55.26 % |
| Rat[1] | 2 mg/kg | i.v. | 1.08 h | 0.08 h | 1606.67 ng/mL | 2020.09 ng·h/mL | 2039.54 ng·h/mL | 1510.95 mL/kg | 1007.89 mL/h/kg | 1.36 h | 1.42 h | / |
Chemical Information
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CAS No. 3044124-79-7
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분자량 363.39
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화학식 C19H18FN7
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SMILES
C[C@@H](C1=CC=C(C=N1)F)NC2=NN3C(C4=NNC(C5CC5)=C4)=CN=C3C=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TRK-IN-32 Related Classifications
HY-175302 Related Classifications
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