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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;

In stock
Item Number
S126376
Grouped product items
SKU Size
Availability
Price Qty
S126376-5mg
5mg
3
$116.90
S126376-10mg
10mg
2
$220.90
S126376-50mg
50mg
2
$574.90

Novel ATP competitive inhibitor of Pim1

Basic Description

Synonyms N-[(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 & Purity Moligand™, ≥98%
Biochemical and Physiological Mechanisms SGI-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 Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action 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;
Note Wherever 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.

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Azoles
Subclass Imidazoles
Intermediate Tree Nodes Substituted imidazoles
Direct Parent Phenylimidazoles
Alternative Parents Phenoxy compounds  Phenol ethers  Secondary alkylarylamines  Aminopyridazines  Piperidines  N-substituted imidazoles  Imidolactams  Heteroaromatic compounds  Trihalomethanes  Trialkylamines  Azacyclic compounds  Hydrocarbon derivatives  Organofluorides  Organooxygen compounds  Organopnictogen compounds  Alkyl fluorides  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents 5-phenylimidazole - 4-phenylimidazole - Phenoxy compound - Phenol ether - Aminopyridazine - Secondary aliphatic/aromatic amine - Monocyclic benzene moiety - N-substituted imidazole - Imidolactam - Benzenoid - Piperidine - Pyridazine - Heteroaromatic compound - Trihalomethane - Tertiary aliphatic amine - Tertiary amine - Azacycle - Secondary amine - Hydrocarbon derivative - Halomethane - Organooxygen compound - Organonitrogen compound - Organofluoride - Organohalogen compound - Organopnictogen compound - Organic oxygen compound - Organic nitrogen compound - Amine - Alkyl fluoride - Alkyl halide - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as phenylimidazoles. These are polycyclic aromatic compounds containing a benzene ring linked to an imidazole ring through a CC or CN bond.
External Descriptors Not available

Associated Targets(Human)

HASPIN Tchem Serine/threonine-protein kinase haspin (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
IRAK3 Tchem Interleukin-1 receptor-associated kinase 3 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PIM1 Tchem Serine/threonine-protein kinase pim-1 (17 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PIM2 Tchem Serine/threonine-protein kinase pim-2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PIM3 Tchem Serine/threonine-protein kinase pim-3 (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRKAG2 Tchem 5'-AMP-activated protein kinase subunit gamma-2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (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)
InChIKey MHXGEROHKGDZGO-UHFFFAOYSA-N
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(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

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Lot Number Certificate Type Date Item
K1520214 Certificate of Analysis May 10, 2023 S126376

Chemical and Physical Properties

Solubility DMSO ≥80mg/mL Water <1.2mg/mL Ethanol ≥80mg/mL
Molecular Weight 405.400 g/mol
XLogP3 4.300
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 8
Rotatable Bond Count 5
Exact Mass 405.178 Da
Monoisotopic Mass 405.178 Da
Topological Polar Surface Area 54.700 Ų
Heavy Atom Count 29
Formal Charge 0
Complexity 529.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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