Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LY2784544(Gandotinib (LY2784544)) 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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
サンプルについてお問い合わせ | |||||
5 mg | 在庫あり | ¥ 11,000 | |||
10 mg | 在庫あり | ¥ 18,500 | |||
25 mg | 在庫あり | ¥ 37,500 | |||
50 mg | 在庫あり | ¥ 72,000 | |||
100 mg | 在庫あり | ¥ 113,500 | |||
500 mg | 在庫あり | ¥ 250,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 12,000 |
説明 | LY2784544(Gandotinib (LY2784544)) 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. |
ターゲット&IC50 | JAK2:3 nM, JAK2 (V617F):0.245 nM(Ki) |
In vitro | In severe combined immunodeficient mice, LY2784544 (administered orally) does not affect CD71/Ter119 positive erythroid progenitor cells within the spleen. LY2784544 significantly inhibits STAT5 phosphorylation in Ba/F3-JAK2 V617F-GFP xenografts (effective dose 50% [ED50]: 12.7 mg/kg). Additionally, in a JAK2 V617F-induced myeloproliferative neoplasm (MPN) model, LY2784544 (administered orally) reduces the tumor burden of Ba/F3-JAK2 V617F-GFP (ED50: 13.7 mg/kg). |
In vivo | In proliferation assays, LY2784544 exhibits an anti-proliferative effect on JAK2 V617F-driven cells, with an IC50 of 68 nM. It demonstrates a less potent effect on cells driven by wild-type JAK2 and JAK3, with IC50 values of 1356 nM and 940 nM, respectively. LY2784544 also inhibits IL-3-activated wild-type JAK2 with an IC50 of 2.26 μM. |
細胞研究 | 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]. |
別名 | LY2784544 |
分子量 | 469.94 |
分子式 | C23H25ClFN7O |
CAS No. | 1229236-86-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 87 mg/mL (185.1 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 9 mg/mL (19.15 mM)
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Gandotinib 1229236-86-5 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors FGFR VEGFR FLT JAK LY2784544 LY-2784544 inhibit LY 2784544 Janus kinase CD135 FLT3 Cluster of differentiation antigen 135 Inhibitor Fms like tyrosine kinase 3 Vascular endothelial growth factor receptor Fibroblast growth factor receptor inhibitor