SML2567

LY2784544

≥98% (HPLC)

• Synonym(e): 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
• Empirische Formel (Hill-System): C₂₃H₂₅ClFN₇O
• CAS-Nummer: 1229236-86-5
• Molekulargewicht: 469.94
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD20482143
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• 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

Beschreibung

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.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable