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.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 2 mg | In stock | $ 116 | |
| 4 mg | In stock | $ 220 | |
| 8 mg | In stock | $ 330 | |
| 20 mg | In stock | $ 644 | |
| 40 mg | In stock | $ 1017 |
| Description | 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. |
| Targets&IC50 | JAK2: 3 nM, JAK2V617F: 0.245 nM(Ki) |
| In vitro | LY2784544 is dissolved in DMSO and stored, and then diluted with appropriate medium before use. 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. |
| Synonyms | LY2784544 |
| CAS No. | 1229236-86-5 |
| Chemical Formula | C23H25ClFN7O |
| Molecular Weight | 469.95 |
| Solubility | Ethanol: 9 mg/mL (19.15 mM) H2O: <1 mg/mL; DMSO: 87 mg/mL (185.1 mM) |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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