JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC 50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity.
性状
Solid
IC50 & Target[1][2]
JAK1 26 nM (IC50) JAK2 0.7 nM (IC50
体外研究(In Vitro)
JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) (TFA) down-regulates p-FLT3 in a dose-dependent manner.JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) (TFA) has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells.JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) (TFA) strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
JAK2/FLT3-IN-1 (30 and 60 mg/kg/day; p.o.; for 14 days) (TFA) exhibits significant antitumor effects. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: NOD/SCID mouse models
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Yang T, et al. Discovery of Potent and Orally Effective Dual JAK2/FLT3 Inhibitors for the Treatment of AcuteMyelogenous Leukemia and Myeloproliferative Neoplasms. J Med Chem. 2019 Oct 31.
溶解度数据
In Vitro: H2O : 33.33 mg/mL (57.31 mM; Need ultrasonic)配制储备液