产品
编 号：F756746
分子式：C29H31F3N8O
分子量：564.6
分子式：C29H31F3N8O
分子量：564.6
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CAS No: 2904690-41-9
产品详情
生物活性：
TRK II-IN-1 is a potent type II TRK inhibitor, with IC50s of 3.3, 6.4, 4.3 and 9.4 nM, for TRKA/B/C and TRKAG667C, respectively. TRK II-IN-1 also inhibits FLT3, RET, and VEGFR2 with IC50s of 1.3, 9.9, and 71.1 nM, respectively. TRK II-IN-1 can be used for the research of TRK driven cancers.
体外研究：
TRK II-IN-1 (compound 12d) (1 μM) demonstrates over 90% of kinase inhibition towards VEGFR2, RET, FLT3 and nearly 70% inhibition against Kit, CSF1R, DDR1 and DDR2.TRK II-IN-1 (72 h) inhibits Ba/F3-CD74-TRKA, Ba/F3-ETV6-TRKB and Ba/F3-ETV6-TRKC cells, with IC50s of 26.1, 44.7 and 15.7 nM, respectively.TRK II-IN-1 (72 h) suppresses proliferation of a panel of Ba/F3 cells stably transformed with wild type, xDFG as well as solvent-front (SF) mutant TRK fusion proteins, with IC50s ranging from 2.6 to 143.3 nM.TRK II-IN-1 (0.4-500 nM; 48 h) induces apoptosis of Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKAG667C cells.TRK II-IN-1 (0.4-500 nM; 24 h) arrests cell cycle progression in the G0/G1 phase in Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKAG667C cells.TRK II-IN-1 (0.8-500 nM; 6 h) suppresses the phosphorylation of TRKA, TRKAG667C kinases, and their downstream AKT, ERK and PLCγ1 in a dose-dependent manner.
TRK II-IN-1 is a potent type II TRK inhibitor, with IC50s of 3.3, 6.4, 4.3 and 9.4 nM, for TRKA/B/C and TRKAG667C, respectively. TRK II-IN-1 also inhibits FLT3, RET, and VEGFR2 with IC50s of 1.3, 9.9, and 71.1 nM, respectively. TRK II-IN-1 can be used for the research of TRK driven cancers.
体外研究：
TRK II-IN-1 (compound 12d) (1 μM) demonstrates over 90% of kinase inhibition towards VEGFR2, RET, FLT3 and nearly 70% inhibition against Kit, CSF1R, DDR1 and DDR2.TRK II-IN-1 (72 h) inhibits Ba/F3-CD74-TRKA, Ba/F3-ETV6-TRKB and Ba/F3-ETV6-TRKC cells, with IC50s of 26.1, 44.7 and 15.7 nM, respectively.TRK II-IN-1 (72 h) suppresses proliferation of a panel of Ba/F3 cells stably transformed with wild type, xDFG as well as solvent-front (SF) mutant TRK fusion proteins, with IC50s ranging from 2.6 to 143.3 nM.TRK II-IN-1 (0.4-500 nM; 48 h) induces apoptosis of Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKAG667C cells.TRK II-IN-1 (0.4-500 nM; 24 h) arrests cell cycle progression in the G0/G1 phase in Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKAG667C cells.TRK II-IN-1 (0.8-500 nM; 6 h) suppresses the phosphorylation of TRKA, TRKAG667C kinases, and their downstream AKT, ERK and PLCγ1 in a dose-dependent manner.
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