1025065-69-3 Usage
Description
SGI-1776 is a potent and selective ATP competitive inhibitor of Pim1, Pim2, and Pim3 kinases, with IC50s of 7 nM, 363 nM, and 69 nM, respectively. It is a PIM inhibitor that has shown potential in various applications due to its ability to target these specific kinases.
Uses
Used in Pharmaceutical Industry:
SGI-1776 is used as a PIM inhibitor for targeting Pim1, Pim2, and Pim3 kinases, which play a role in various cellular processes, including cell proliferation, survival, and differentiation. Its potent inhibition of these kinases makes it a valuable compound in the development of therapeutic strategies for cancer and other diseases.
Used in Cancer Research:
SGI-1776 is used as a research tool for studying the role of Pim kinases in cancer cell growth and survival. By inhibiting these kinases, researchers can gain insights into the molecular mechanisms underlying cancer progression and identify potential therapeutic targets for the development of novel anticancer drugs.
Used in Drug Development:
SGI-1776 is used as a lead compound in the development of new drugs targeting Pim kinases. Its potent and selective inhibition of Pim1, Pim2, and Pim3 makes it an attractive starting point for the design and synthesis of more effective and specific inhibitors for therapeutic applications.
Used in Drug Delivery Systems:
Similar to gallotannin, SGI-1776 can also benefit from novel drug delivery systems to enhance its applications and efficacy against cancer cells. Various organic and metallic nanoparticles can be employed as carriers for SGI-1776 delivery, aiming to improve its delivery, bioavailability, and therapeutic outcomes.
Biological Activity
sgi-1776 free base, n-((1-methylpiperidin-4-yl)methyl)-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-amine, is a potent atp-competitive inhibitor of the serine/threonine family of pim kinase, an enzyme regulating cell survival. through extensive biomedical characterization, sgi-1776 exhibits specificity to the three isoforms of the pim family, including pim-1, pim-2, and pim-3. according to preliminary results from studies treating prostate cancer cells, sgi-1776 dose-dependently reduces phosphorylation of known pim kinase substrates involved in cell cycle progression and apotosis (p21cip1/waf1 and bad), compromises overall cell viability by inducing g1 cell cycle arrest and triggering apoptosis, and reduces cell viability in a multidrug resistance 1 (mdr1) protein based taxane-refractory prostate cancer cell line.shannon m. mumenthaler, patricia y.b. ng, amanda hodge, davide bearss, gregory berk, sarath kanekal, sanjeev redkar, pietro taverna, davide b. agus, and anjali jain. pharmacological inhibition of pim kinases alters prostate cancer cell growth and resensitizes chemoresistant cells to taxanes. mol cancer ther. 2009; 8(10): 2882-2893lisa s. chen, s anjeev redkar, david bearss, william g. wierda and varsha gandhi. pim kinase inhibitor, sgi-1776, induces apoptosis in cll lymphocytes. blood. 2009; 114(19): 4150-4157
Check Digit Verification of cas no
The CAS Registry Mumber 1025065-69-3 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,2,5,0,6 and 5 respectively; the second part has 2 digits, 6 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 1025065-69:
(9*1)+(8*0)+(7*2)+(6*5)+(5*0)+(4*6)+(3*5)+(2*6)+(1*9)=113
113 % 10 = 3
So 1025065-69-3 is a valid CAS Registry Number.
1025065-69-3Relevant articles and documents
IMIDAZO[1,2-B]PYRIDAZINE AND PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS
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Page/Page column 54-55, (2008/12/05)
The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II), or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer and other Pim kinase-associated conditions are also disclosed.
