产品
编 号：F752999
分子式：C22H18F2N4
分子量：376.4
分子式：C22H18F2N4
分子量：376.4
产品类型
规格
价格
是否有货
结构图
CAS No: 2460924-63-2
产品详情
生物活性：
Trk-IN-20 is a kind of 3-vinylindazole derivatives. Trk-IN-20 suppresses Trk kinases functions by phosphorylation inhibition of TrkA/B/C with IC50 values of 1.6 nM, 2.9 nM and 2.0 nM, respectively.
体内研究：
Trk-IN-20 (compound 7mb) (p.o.; 10 mg/kg) shows short half-life of 1.39 hours and a low oral bioavailability of 8.79% in rats.Animal Model:Pharmacokinetic Profile of Trk-IN-20 (Compound 7mb) in Rats
Dosage:
Administration:
Result:RouteDose (mg/kg)AUC0-∞ (μM.h)Cmax (μM)T1/2 (h)CL (L/h/kg)BA (%)
i.v.23.696.771.391.44/
p.o.101.620.361.13-8.79
体外研究：
NTRK1 is a proto-oncogene in colon cancer, Trk inhibitors have been detected to against a variety of human cancers.Trk-IN-20 (compound 7mb) (0.031, or 0.018 μM, respectively; 72 h) exhibits strong inhibition against the Larotrectinib-resistant cells with NTRK1-G667C or NTRK3-G696A mutations with IC50s of 0.031 and 0.018 μM, respectively.Trk-IN-20 (compound 7mb) (9-22 nM; 72 h) inhibits BaF3 murine cells stably transformed with NTRK oncogenic fusions including CD74-NTRK1, ETV6-NTRK2 and ETV6-NTRK3 with IC50s of 15, 22, and 9 nM, respectively.Trk-IN-20 (compound 7mb) (0.32, 1.6, 8, 40, 200; 6 h) inhibits activation of Trk and its downstream proteins in BaF3-CD74-NTRK1, BaF3-ETV6-NTRK2, BaF3-ETV6-NTRK3 cells.Trk-IN-20 (compound 7mb) tightly bound to ATP-binding site of TrkA, TrkB, and TrkC with binding constant (Kd) values of 1.6, 3.1 and 4.9 nM, respectively.
Trk-IN-20 is a kind of 3-vinylindazole derivatives. Trk-IN-20 suppresses Trk kinases functions by phosphorylation inhibition of TrkA/B/C with IC50 values of 1.6 nM, 2.9 nM and 2.0 nM, respectively.
体内研究：
Trk-IN-20 (compound 7mb) (p.o.; 10 mg/kg) shows short half-life of 1.39 hours and a low oral bioavailability of 8.79% in rats.Animal Model:Pharmacokinetic Profile of Trk-IN-20 (Compound 7mb) in Rats
Dosage:
Administration:
Result:RouteDose (mg/kg)AUC0-∞ (μM.h)Cmax (μM)T1/2 (h)CL (L/h/kg)BA (%)
i.v.23.696.771.391.44/
p.o.101.620.361.13-8.79
体外研究：
NTRK1 is a proto-oncogene in colon cancer, Trk inhibitors have been detected to against a variety of human cancers.Trk-IN-20 (compound 7mb) (0.031, or 0.018 μM, respectively; 72 h) exhibits strong inhibition against the Larotrectinib-resistant cells with NTRK1-G667C or NTRK3-G696A mutations with IC50s of 0.031 and 0.018 μM, respectively.Trk-IN-20 (compound 7mb) (9-22 nM; 72 h) inhibits BaF3 murine cells stably transformed with NTRK oncogenic fusions including CD74-NTRK1, ETV6-NTRK2 and ETV6-NTRK3 with IC50s of 15, 22, and 9 nM, respectively.Trk-IN-20 (compound 7mb) (0.32, 1.6, 8, 40, 200; 6 h) inhibits activation of Trk and its downstream proteins in BaF3-CD74-NTRK1, BaF3-ETV6-NTRK2, BaF3-ETV6-NTRK3 cells.Trk-IN-20 (compound 7mb) tightly bound to ATP-binding site of TrkA, TrkB, and TrkC with binding constant (Kd) values of 1.6, 3.1 and 4.9 nM, respectively.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备