SGI-1776

• CAT Number: I000164
• CAS Number: 1025065-69-3
• Molecular Formula: C₂₀H₂₂F₃N₅O
• Molecular Weight: 405.42
• Purity: ≥95%
• Target: Pim
• Solubility: 10 mM in DMSO
• Storage: 3 years -20℃ powder
• IC50: 7 nM [1]
• IUPAC Name: N-[(1-methylpiperidin-4-yl)methyl]-3-[3-(trifluoromethoxy)phenyl]imidazo[1,2-b]pyridazin-6-amine
• InChI: InChI=1S/C20H22F3N5O/c1-27-9-7-14(8-10-27)12-24-18-5-6-19-25-13-17(28(19)26-18)15-3-2-4-16(11-15)29-20(21,22)23/h2-6,11,13-14H,7-10,12H2,1H3,(H,24,26)
• InChIKey: MHXGEROHKGDZGO-UHFFFAOYSA-N
• SMILES: CN1CCC(CC1)CNC2=NN3C(=NC=C3C4=CC(=CC=C4)OC(F)(F)F)C=C2

SGI-1776 (Cat.No:I000164) is a small molecule inhibitor that targets the enzyme Pim kinase. Pim kinases play a role in promoting cell survival and proliferation in cancer cells. SGI-1776 has shown potential in preclinical studies as an anticancer agent, inhibiting tumor growth and enhancing the efficacy of chemotherapy in certain cancer types.

Reference

1:Biochemical changes of salivary gland adenoid cystic carcinoma cells induced by SGI-1776. Hou X, Yu Y, Feng J, Wang J, Zheng C, Ling Z, Ge M, Zhu X.Exp Cell Res. 2017 Mar 15;352(2):403-411. doi: 10.1016/j.yexcr.2017.02.029. Epub 2017 Feb 20. PMID: 28228352 Free Article2:The novel anti-adipogenic effect and mechanisms of action of SGI-1776, a Pim-specific inhibitor, in 3T3-L1 adipocytes. Park YK, Hong VS, Lee TY, Lee J, Choi JS, Park DS, Park GY, Jang BC.Int J Mol Med. 2016 Jan;37(1):157-64. doi: 10.3892/ijmm.2015.2415. Epub 2015 Nov 19. PMID: 26719859 3:SGI-1776, an imidazo pyridazine compound, inhibits the proliferation of ovarian cancer cells by inactivating Pim-1. Xie J, Bai J.Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2014 Jul;39(7):649-57. doi: 10.11817/j.issn.1672-7347.2014.07.001. PMID: 25080901 Free Article4:Combination of Pim kinase inhibitor SGI-1776 and bendamustine in B-cell lymphoma. Yang Q, Chen LS, Neelapu SS, Gandhi V.Clin Lymphoma Myeloma Leuk. 2013 Sep;13 Suppl 2:S355-62. doi: 10.1016/j.clml.2013.05.024. PMID: 24290221 Free PMC Article5:Biological effects of the Pim kinase inhibitor, SGI-1776, in multiple myeloma. Cervantes-Gomez F, Chen LS, Orlowski RZ, Gandhi V.Clin Lymphoma Myeloma Leuk. 2013 Sep;13 Suppl 2:S317-29. doi: 10.1016/j.clml.2013.05.019. Epub 2013 Aug 27. PMID: 23988451 Free PMC Article6:The Pim kinase inhibitor SGI-1776 decreases cell surface expression of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and drug transport by Pim-1-dependent and -independent mechanisms. Natarajan K, Bhullar J, Shukla S, Burcu M, Chen ZS, Ambudkar SV, Baer MR.Biochem Pharmacol. 2013 Feb 15;85(4):514-24. doi: 10.1016/j.bcp.2012.12.006. Epub 2012 Dec 19. PMID: 23261525 Free PMC Article7:Transcription and translation are primary targets of Pim kinase inhibitor SGI-1776 in mantle cell lymphoma. Yang Q, Chen LS, Neelapu SS, Miranda RN, Medeiros LJ, Gandhi V.Blood. 2012 Oct 25;120(17):3491-500. doi: 10.1182/blood-2012-02-412643. Epub 2012 Sep 6. PMID: 22955922 Free PMC Article8:The FLT3 and Pim kinases inhibitor SGI-1776 preferentially target FLT3-ITD AML cells. Hospital MA, Green AS, Lacombe C, Mayeux P, Bouscary D, Tamburini J.Blood. 2012 Feb 16;119(7):1791-2. doi: 10.1182/blood-2011-11-393066. No abstract available. PMID: 22343664 Free Article9:Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program. Batra V, Maris JM, Kang MH, Reynolds CP, Houghton PJ, Alexander D, Kolb EA, Gorlick R, Keir ST, Carol H, Lock R, Billups CA, Smith MA.Pediatr Blood Cancer. 2012 Oct;59(4):749-52. doi: 10.1002/pbc.23364. Epub 2011 Nov 2. PMID: 22052829 Free PMC Article10:Mechanisms of cytotoxicity to Pim kinase inhibitor, SGI-1776, in acute myeloid leukemia. Chen LS, Redkar S, Taverna P, Cortes JE, Gandhi V.Blood. 2011 Jul 21;118(3):693-702. doi: 10.1182/blood-2010-12-323022. Epub 2011 May 31. PMID: 21628411 Free PMC Article