1173928-26-1
Chemical Structure
SGI-1776
- CAS No.: 1173928-26-1
- Formula:C20H26F3N5O9S2
- Molecular Weight:601.57
IUPAC Name: N-((1-methylpiperidin-4-yl)methyl)-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-amine bis(sulfate)
InChIKey: VUAYTLGZIBSISZ-UHFFFAOYSA-N
SMILES: CN1CCC(CC1)CNC2=NN3C(C=C2)=NC=C3C4=CC=CC(OC(F)(F)F)=C4.O=S(O)(O)=O.O=S(O)(O)=O
Biological Activity: SGI-1776 is an orally active Pim kinase and FLT3 inhibitor with IC50 values of 7 nM, 363 nM, 69 nM, and 44 nM for Pim-1, Pim-2, Pim-3, and FLT3, respectively. SGI-1776 downregulates C/EBP-α, PPAR-γ, FAS, Leptin, and RANTES, and decreases STAT-3 phosphorylation. SGI-1776 induces Apoptosis, cell cycle arrest, mitochondrial depolarization, and reduces RNA synthesis, protein synthesis, and Mcl-1. SGI-1776 inhibits adipogenesis and lipid accumulation. SGI-1776 has anticancer activity against leukemia[1][2][3][4][5][6][7][8][9].
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SGI-1776 | SGI-1776 is an orally active Pim kinase and FLT3 inhibitor with IC50 values of 7 nM, 363 nM, 69 nM, and 44 nM for Pim-1, Pim-2, Pim-3, and FLT3, respectively. SGI-1776 downregulates C/EBP-α, PPAR-γ, FAS, Leptin, and RANTES, and decreases STAT-3 phosphorylation. SGI-1776 induces Apoptosis, cell cycle arrest, mitochondrial depolarization, and reduces RNA synthesis, protein synthesis, and Mcl-1. SGI-1776 inhibits adipogenesis and lipid accumulation. SGI-1776 has anticancer activity against leukemia. | |||||||||||||||||||||
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References
- [1]. Park YK, et al. The novel anti-adipogenic effect and mechanisms of action of SGI-1776, a Pim-specific inhibitor, in 3T3-L1 adipocytes. International Journal of Molecular Medicine. 2016 Jan 1;37(1):157-64. [Content Brief]
- [2]. Chen LS, et al. Mechanisms of cytotoxicity to Pim kinase inhibitor, SGI-1776, in acute myeloid leukemia. Blood. 2011 Jul 21;118(3):693-702. [Content Brief]
- [3]. Hou X, et al. Biochemical changes of salivary gland adenoid cystic carcinoma cells induced by SGI-1776. Experimental cell research. 2017 Mar 15;352(2):403-411. [Content Brief]
- [4]. Chen Q, et al. The Mechanisms of PIM Kinase Inhibitor, SGI-1776 Free Base, in Treating Myeloma-Associated Bone Disease. Blood. 2017 Dec 8;130:3079.
- [5]. Brown VI, et al. Inhibiting PIM-1 Is Effective in Vitro and in Vivo against ALL: A Novel Mechanistic and Potentially Clinically Relevant Druggable Target. Blood. 2008 Nov 16;112(11):1922.
- [6]. Lampron MC, et al. Pim1: A New Dna Repair Modulator Implicated in Pulmonary Hypertension. Circulation. 2017 Nov 14;136(suppl_1):A16978-.
- [7]. Kelly KR, et al. Targeting PIM kinase activity with the novel small molecule inhibitor SGI-1776 significantly augments the efficacy of cytarabine in models of acute myeloid leukemia. Blood. 2010 Nov 19;116(21):3253.
- [8]. Chen LS, et al. Pim kinase inhibitor, SGI-1776, induces apoptosis in acute myeloid leukemia primary cells. Cancer Research. 2010 Apr 15;70(8_Supplement):1649-.
- [9]. Yang Q, et al. Targeting Pim kinases by SGI-1776 in mantle cell lymphoma. Cancer Research. 2011 Apr 15;71(8_Supplement):586-.
