SML2567
LY2784544
≥98% (HPLC)
别名:
3-(4-Chloro-2-fluorobenzyl)-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine, 3-[(4-Chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)imidazo[1,2-b]pyridazin-6-amine, LY 2784544, LY-2784544
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关于此项目
经验公式（希尔记法）:
C23H25ClFN7O
化学文摘社编号:
分子量:
469.94
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
Fc1c(ccc(c1)Cl)Cc2[n]3c(nc2C)C(=CC(=N3)Nc5n[nH]c(c5)C)CN4CCOCC4
InChI
1S/C23H25ClFN7O/c1-14-9-21(29-28-14)27-22-11-17(13-31-5-7-33-8-6-31)23-26-15(2)20(32(23)30-22)10-16-3-4-18(24)12-19(16)25/h3-4,9,11-12H,5-8,10,13H2,1-2H3,(H2,27,28,29,30)
InChI key
SQSZANZGUXWJEA-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
composition
H2O, 0-4 mol/mol (moles per mole of product)
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
LY2784544 is an orally active, ATP-competitive, potent and JAK2-selective janus tyrosine kinase inhibitor (IC50/[ATP] = 2.52 nM/5 μM/JAK2, 19.8 nM/20 μM/JAK1, 48.0 nM/2 μM/JAK3) with little activity toward 79 other kinases. LY2784544 selectively inhibits signaling/proliferation driven by oncogenic JAK2V617F (IC50 = 20/55 nM) over those mediated by wt JAK2 upon IL-3 induction (IC50 = 1183/1309 nM) in Ba/F3 cultures and displays in vivo efficacious in a JAK2V617F-induced murine MPN model (10-80 mg/kg bid po.). LY2784544 is also reported to display Zn-dependent (optimal [Zn+2] = 100 μM) GPR39 agonist activity, but not 11 other GPRs.
Orally active, ATP-competitive, potent and JAK2-selective janus tyrosine kinase inhibitor with additional Zn+2-dependent GPR39 agonist activity.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Wei Zhou et al.
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L Ma et al.
Blood cancer journal, 3, e109-e109 (2013-04-16)
Owing to the prevalence of the JAK2V617F mutation in myeloproliferative neoplasms (MPNs), its constitutive activity, and ability to recapitulate the MPN phenotype in mouse models, JAK2V617F kinase is an attractive therapeutic target. We report the discovery and initial characterization of
Nuramalina H Mumin et al.
BMC cancer, 19(1), 102-102 (2019-01-27)
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Seiji Sato et al.
Molecular pharmacology, 90(6), 726-737 (2016-11-03)
In this study, we identified two previously described kinase inhibitors-3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(3-methyl-1H-pyrazol-5-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine (LY2784544) and 1H-benzimidazole-4-carboxylic acid, 2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-(4-morpholinyl)- (GSK2636771)-as novel GPR39 agonists by unbiased small-molecule-based screening using a β-arrestin recruitment screening approach (PRESTO-Tango). We characterized the signaling of LY2784544 and GSK2636771 and compared
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