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;

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

SynonymsN-[(1-methylpiperidin-4-yl)methyl]-3-[3-(trifluoromethoxy)phenyl]imidazo[2,1-f]pyridazin-6-amine | Imidazo[1,2-b]pyridazin-6-amine, N-[(1-methyl-4-piperidinyl)methyl]-3-[3-(trifluoromethoxy)phenyl]- | NSC800883 | NSC-800883 | SB19298 | AC-28432 | N-((1-Me
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsSGI-1776 is a novel ATP-competitive inhibitor of Pim-1, Pim-2, and Pim-3 (IC50 = 7, 363, and 69 nM, respectively). In addition to inhibiting Pim, this compound also inhibits FLT3 (IC50 = 44 nM). SGI-1776 is also cytotoxic in AML primary cells, regardless
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;
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Refer to SDS for further information. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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(Human)

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

Certificates

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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