Gandotinib 是一种JAK2抑制剂，IC50为 3 nM。它也抑制FLT3、FLT4、FGFR2、TYK2 和 TRKB，IC50分别为 4、25、32、44 和 95 nM。

LY2784544(Gandotinib) is a potent JAK2 inhibitor (IC50: 3 nM), effective in JAK2V617F(Ki: 0.245 nM). The selectivity is higher 8- and 20-fold than JAK1 and JAK3.

作用于在患有重症联合免疫缺陷小鼠的脾脏中,LY2784544（p.o.）不影响CD71/Ter119 阳性红系祖细胞.LY2784544对Ba/F3-JAK2 V617F-GFP移植瘤中的STAT5磷酸化有显著抑制效果（TED50：12.7 mg/kg）.在JAK2 V617F诱导的MPN模型中,LY2784544（p.o.）还减少Ba/F3-JAK2 V617F-GFP肿瘤负担（TED50：13.7 mg/kg）.

在增殖实验中, LY2784544对JAK2 V617F驱动的细胞具有抗增殖效应（IC50：68 nM）；对野生型JAK2驱动细胞的IC50为1356 nM；对JAK3驱动细胞的IC50为940 nM。LY2784544对IL-3激活的野生型JAK2也有抑制作用（IC50：2.26 μM）。

LY2784544 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. Ba/F3 cells expressing JAK2V617F are placed in RPMI-1640-containing vehicle (DMSO) or LY2784544 (concentration range, 0.001-20 μM) (1×104 cells/96-well). Ba/F3 cells expressing wild-type JAK2 are treated similarly except IL-3 (2 ng/mL) is added. After a 72-hour incubation, cell proliferation is assessed by adding Cell Titer 96 Aqueous One Solution Reagent (20 μL/well). The IC50 for inhibition of cell proliferation is calculated using the GraphPad Prism 4 software[1].

1229236-86-5

C23H25ClFN7O

469.95

LY2784544

DMSO:87 mg/mL (185.1 mM)
H2O:<1 mgml
Ethanol:9 mg/mL (19.15 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years