TIY-7
TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKAG595R, TRKAG667C, TRKAF589L, TRKCG623R, TRKCG696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model.
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- No. CAS: 2846435-83-2
- Fòrmula: C21H18F4N6O
- Peso molecular:446.40
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
TrkA 2.9 nM (IC50) |
TrkA |
TrkC |
In Vitro
TIY-7 (compound 12c) shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKAG595R, TRKAG667C, TRKAF589L, TRKCG623R, TRKCG696A, respectively[1].
TIY-7 (1 µM) shows selectivity with inhibitory rate of 62%, 99%, 11% for ALK, ROS1, and JAK1 kinase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
TIY-7 (30 mg/kg; P.o.; twice daily for 12-14 consecutive days) inhibits tumor progression in a dose-dependent manner in xenograft model[1].
Pharmacokinetic Parameters of TIY-7 in Male Sprague-Dawley rats[1].
| Dose (mg/kg) | Cmax (ng/mL) | Tmax (h) | T1/2 (h) | CL (mL/min/kg) | F % | MRT0-t (h) | AUCtot (ng/mL·h) | AUCextra (%) | |
| ip mice | 9.103 | 2078 | 0.0833 | 0.8 | 154 | 86 | 0.7 | 982.3 | 1.3 |
| iv mice | 0.711 | 322.7 | 0.0833 | 1.1 | 133 | 0.9 | 88.8 | 15.2 | |
| iv dog | 26.76 | 272 (µg/mL) | 0.0833 | 3.8 | 0.69 | 3.8 | 654.7 (µg/mL·h) | 0.9 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats[1]
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Dosage:5 mg/kg for p.o.; 1 mg/kg for i.v.
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Administration:P.o. or i.v.
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Result:Showed good PK properties with an oral bioavailability (F) of 39.8%.
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Animal Model:6-week-old BALB/cA nude mice (BaF3-TMP3-TRKA-WT and BaF3-ETV6-TRKC-G623R xenograft models)[1]
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Dosage:30 mg/kg (dissolved in 70% PEG400 and 30% water)
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Administration:P.o.; twice daily; 12-14 consecutive days
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Result:Dose-dependently inhibited tumor progression with the TGI of 95% and 86% in BaF3-TMP3-TRKA-WT and BaF3-ETV6-TRKC-G623R xenograft model.
Chemical Information
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No. CAS 2846435-83-2
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Peso molecular 446.40
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Fòrmula C21H18F4N6O
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SMILES
FC1=CC=C(C([C@H]2CCCN2C3=NC4=C(C=NN4C=C3)C5=CNN=C5)=C1)OCC(F)(F)F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TIY-7 Related Classifications
HY-146755 Related Classifications
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