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.
|Source||Clin Lymphoma Myeloma Leuk (2013). Figure 2. SGI-1776|
|Method||Macromolecule synthesis assay|
|Cell Lines||JeKo-1 cells|
|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.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Transcription and translation are primary targets of Pim kinase inhibitor, SGI-1776, in mantle cell lymphoma.
Yang Q, et al. Blood. 2012 Sep 6. PMID: 22955922.
Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program.
Batra V, et al. Pediatr Blood Cancer. 2012 Oct;59(4):749-52. PMID: 22052829.
Mechanisms of cytotoxicity to Pim kinase inhibitor, SGI-1776, in acute myeloid leukemia.
Chen LS, et al. Blood. 2011 Jul 21;118(3):693-702. PMID: 21628411.
Pim kinase inhibitor, SGI-1776, induces apoptosis in chronic lymphocytic leukemia cells.
Chen LS, et al. Blood. 2009 Nov 5;114(19):4150-7. PMID: 19734450.
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