产品
编 号：F756329
分子式：C21H18F4N6O
分子量：446.4
分子式：C21H18F4N6O
分子量：446.4
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CAS No: 2846435-83-2
产品详情
生物活性：
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.
体内研究：
TIY-7 (5 mg/kg for p.o.; 1 mg/kg for i.v.) shows good oral bioavailability (F) of 39.8%.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.Pharmacokinetic Parameters of TIY-7 in Male Sprague-Dawley rats.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 mice9.10320780.08330.8154860.7982.31.3
iv mice0.711322.70.08331.11330.988.815.2
iv dog26.76272 (μg/mL)0.08333.80.693.8654.7 (μg/mL·h)0.9
Male Sprague-Dawley rats; 5 mg/kg for p.o.; 1 mg/kg for i.v..Animal Model:Male Sprague-Dawley rats
Dosage:5 mg/kg for p.o.; 1 mg/kg for i.v.
Administration:P.o. or i.v.
Result:Showed good PK properties with an oral bioavailability (F) of 39.8%.
Animal Model:6-week-old BALB/cA nude mice (BaF3-TMP3-TRKA-WT and BaF3-ETV6-TRKC-G623R xenograft models)
Dosage:30 mg/kg (dissolved in 70% PEG400 and 30% water)
Administration:P.o.; twice daily; 12-14 consecutive days
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.
体外研究：
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.TIY-7 (1 μM) shows selectivity with inhibitory rate of 62%, 99%, 11% for ALK, ROS1, and JAK1 kinase.
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.
体内研究：
TIY-7 (5 mg/kg for p.o.; 1 mg/kg for i.v.) shows good oral bioavailability (F) of 39.8%.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.Pharmacokinetic Parameters of TIY-7 in Male Sprague-Dawley rats.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 mice9.10320780.08330.8154860.7982.31.3
iv mice0.711322.70.08331.11330.988.815.2
iv dog26.76272 (μg/mL)0.08333.80.693.8654.7 (μg/mL·h)0.9
Male Sprague-Dawley rats; 5 mg/kg for p.o.; 1 mg/kg for i.v..Animal Model:Male Sprague-Dawley rats
Dosage:5 mg/kg for p.o.; 1 mg/kg for i.v.
Administration:P.o. or i.v.
Result:Showed good PK properties with an oral bioavailability (F) of 39.8%.
Animal Model:6-week-old BALB/cA nude mice (BaF3-TMP3-TRKA-WT and BaF3-ETV6-TRKC-G623R xenograft models)
Dosage:30 mg/kg (dissolved in 70% PEG400 and 30% water)
Administration:P.o.; twice daily; 12-14 consecutive days
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.
体外研究：
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.TIY-7 (1 μM) shows selectivity with inhibitory rate of 62%, 99%, 11% for ALK, ROS1, and JAK1 kinase.
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