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SGI-1776 free base - ≥98%, high purity , CAS No.1025065-69-3, Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of histone H3 associated protein kinase;Inhibitor of Pim-1 proto-oncogene; serine/threonine kinase;Inhibitor of Pim-2 proto-oncogene; serine/threonine kinase;Inhibitor of Pim-3 proto-oncogene;

  • Moligand™
  • ≥98%
Item Number
S126376
Grouped product items
SKUSizeAvailabilityPrice Qty
S126376-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$116.90
S126376-10mg
10mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$220.90
S126376-50mg
50mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$574.90

Novel ATP competitive inhibitor of Pim1

Basic Description

SynonymsSGI-1776|1025065-69-3|SGI-1776 free base|N-[(1-methylpiperidin-4-yl)methyl]-3-[3-(trifluoromethoxy)phenyl]imidazo[1,2-b]pyridazin-6-amine|SGI1776|N-((1-methylpiperidin-4-yl)methyl)-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-amine|SGI 1776|N-[
Specifications & Purity≥98%
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of fms related receptor tyrosine kinase 3;Inhibitor of histone H3 associated protein kinase;Inhibitor of Pim-1 proto-oncogene; serine/threonine kinase;Inhibitor of Pim-2 proto-oncogene; serine/threonine kinase;Inhibitor of Pim-3 proto-oncogene;
Product Description

SGI-1776 is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin
A potent apoptotic that targets Pim and FLT3 in AML and CLL cells.

Associated Targets

HASPIN Tchem Serine/threonine-protein kinase haspin 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

IRAK3 Tchem Interleukin-1 receptor-associated kinase 3 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIM1 Tchem Serine/threonine-protein kinase pim-1 17 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIM2 Tchem Serine/threonine-protein kinase pim-2 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIM3 Tchem Serine/threonine-protein kinase pim-3 3 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKAG2 Tchem 5'-AMP-activated protein kinase subunit gamma-2 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 3 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

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)
InChi Key MHXGEROHKGDZGO-UHFFFAOYSA-N
Canonical SMILES CN1CCC(CC1)CNC2=NN3C(=NC=C3C4=CC(=CC=C4)OC(F)(F)F)C=C2
Isomeric SMILES CN1CCC(CC1)CNC2=NN3C(=NC=C3C4=CC(=CC=C4)OC(F)(F)F)C=C2
PubChem CID 24795070
Molecular Weight 405.42

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Certificate of Analysis(COA)

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Lot NumberCertificate TypeDateItem
K1520214Certificate of AnalysisMay 10, 2023 S126376

Chemical and Physical Properties

SolubilityDMSO ≥80mg/mL Water <1.2mg/mL Ethanol ≥80mg/mL

Related Documents

References

1. Drygin D, Haddach M, Pierre F, Ryckman DM.  (2012)  Potential use of selective and nonselective Pim kinase inhibitors for cancer therapy..  J Med Chem,  55  (19): (8199-208).  [PMID:22924342]
2. Cervantes-Gomez F, Chen LS, Orlowski RZ, Gandhi V.  (2013)  Biological effects of the Pim kinase inhibitor, SGI-1776, in multiple myeloma..  Clin Lymphoma Myeloma Leuk,  13 Suppl 2  (3): (S317-29).  [PMID:23988451]

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