TRK-IN-31
TRK-IN-31 is an orally active TRK inhibitor with an IC50 of 1.8 nM. TRK-IN-31 has superior antiproliferative activity in the Ba/F3-MPRIP-TRKAG667C cells, and potently inhibits TRK kinase activity with high selectivity. TRK-IN-31 significantly inhibits tumor growth in Ba/F3-MPRIP-TRKAG667C subcutaneous tumor mice model.
For research use only. We do not sell to patients.
- Formula: C30H29F2N5O4
- Molecular Weight:561.58
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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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TRK 1.8 nM () |
TRK-IN-31 (Compound 10o) (72 h) has potent antiproliferative activity with IC50s of 81.4 and 131.4 nM for Ba/F3-MPRIP-TRKAG667C and Ba/F3-MPRIP-TRKAG595R cells, respectively[1].
TRK-IN-31 (1-20 nM, 2 h) notably inhibits TRK signaling in both Ba/F3-MPRIP-TRKA and MO-91 cells[1].
TRK-IN-31 (0.04-1 μM, 2 h) significantly inhibits cellular TRKA G667C signaling with great efficacy at 0.2 μM in Ba/F3-MPRIP-TRKAG667C cells[1].
TRK-IN-31 (1 μM, 1 h) has great selectivity among a panel of 92 kinases (S(10): 0.043) and significant inhibitory activities against TRKA/B/C and CSF1R with inhibition rates of 97%-103%[1].
TRK-IN-31 has superior binding capacity on TRKAG595R, enhances stability with protein and reduces conformational fluctuations[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-MPRIP-TRKA cells, MO-91 cells
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Concentration:1, 5, 20 nM
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Incubation Time:2 h
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Result:Notably inhibited TRK signaling in both Ba/F3-MPRIP-TRKA and MO-91 cells.
Nearly abolished the activation of TRKA and its key downstream molecules PLCγ and Erk at 5 nmol/L in Ba/F3-MPRIP-TRKA cells.
| Species | Dose | Route | Tmax | Cmax | AUC0-t | AUC0-∞ | MRT | T1/2 |
|---|---|---|---|---|---|---|---|---|
| Mice | 10 mg/kg | p.o. | 2 h | 36.8 ng/mL | 0.151 ng/L.h | 0.201 ng/L.h | 6.04 h | 3.48 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice (4-6 weeks old) were injected subcutaneously into the right flank with Ba/F3-MPRIP-TRKAG667C cells (2 × 106 cells/mouse)[1].
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Dosage:25, 150 mg/kg
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Administration:Oral gavage (p.o.), twice daily for 10 days after tumors reaching approximately 50 mm3.
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Result:Significantly delayed tumor growth in a dose-dependent manner, with inhibition rates of 42.4% and 52.5% at 25 and 150 mg/kg, respectively.
Had good tolerance with no significant body weight loss up to 150 mg/kg.
Chemical Information
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Molecular Weight 561.58
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Formula C30H29F2N5O4
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SMILES
FC1=CC=C(C=C1[C@@H]2N(C3=CNC(C(C(NC4=CC5=C(C=C4)OC(C(N6CCN(CC6)C)=O)=C5)=O)=C3)=O)CCC2)F
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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)
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