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SML2567

LY2784544

≥98% (HPLC)

Synonym(s):

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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About This Item

Empirical Formula (Hill Notation):
C23H25ClFN7O
CAS Number:
1229236-86-5
Molecular Weight:
469.94
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD20482143
Assay:
≥98% (HPLC)
Form:
powder
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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

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

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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