SGI-1776 is novel small molecule inhibitor of PIM kinase activity with IC50 of 7 ± 1.8, 363 ± 27.6 and 69 ± 9.2 nM for Pim-1, Pim-2, and Pim-3, respectively.SGI-1776 compound is a FLT3 kinase inhibitor and preferentially induces apoptosis in AML cells harboring a FLT3-IT3 mutation.SGI-1776 also exhibited cytotoxic activity in vitro with a median relative IC50 of 3.1μM.
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Source | Clin Lymphoma Myeloma Leuk (2013). Figure 2. SGI-1776 |
| Method | Macromolecule synthesis assay | |
| Cell Lines | JeKo-1 cells | |
| Concentrations | 5 μM | |
| Incubation Time | 24 h | |
| Results | With 5μM SGI-1776 alone there was 20% reduction of DNA synthesis level compared to DMSO treated control cells, while 40%-65% reduction of DNA synthesis was induced by 5 and 10μM of bendamustine single treatment in 24hr. |
| Molecular Weight | 405.42 |
| Formula | C20H22F3N5O |
| CAS Number | 1025065-69-3 |
| Solubility (25°C) | DMSO 65 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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