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SGI-1776

Cat. No. M1779
SGI-1776 Structure
Size Price Availability Quantity
10mg USD 200 In stock
50mg USD 495 In stock
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Quality Control
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 405.42
Formula C20H22F3N5O
CAS Number 1025065-69-3
Purity 98.55%
Solubility DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SGI-1776 supplier, Pim, inhibitors

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