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LY 2784544

Basic information Safety Supplier Related

LY 2784544 Basic information

Product Name:
LY 2784544
Synonyms:
  • LY 2784544
  • 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
  • 3-(4-chloro-2-fluorobenzyl)-2-Methyl-N-(3-Methyl-1H-pyrazol-5-yl)-8-(MorpholinoMethyl)iMidazo[1,2-b]pyridazin-6-aMine
  • LY2784544/LY-2784544
  • 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)-
  • LY2874544
  • CS-13
  • Gandotinib (LY2784544)
CAS:
1229236-86-5
MF:
C23H25ClFN7O
MW:
469.94
Product Categories:
  • Inhibitors
  • JAK
  • STAT
  • Inhibitor
  • JAK/STAT
Mol File:
1229236-86-5.mol
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LY 2784544 Chemical Properties

Density 
1.45
storage temp. 
Store at -20°C
solubility 
≥23.5 mg/mL in DMSO; insoluble in H2O; ≥5.65 mg/mL in EtOH with gentle warming and ultrasonic
form 
solid
pka
14.12±0.10(Predicted)
color 
Light yellow to yellow
InChIKey
SQSZANZGUXWJEA-UHFFFAOYSA-N
SMILES
C12=NC(C)=C(CC3=CC=C(Cl)C=C3F)N1N=C(NC1C=C(C)NN=1)C=C2CN1CCOCC1
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LY 2784544 Usage And Synthesis

Uses

LY2784544 is a JAK2 inhibitor. LY2784544 may be used as a potential treatment for patients with myeloproliferative neoplasm.

Definition

ChEBI: Gandotinib is a member of pyridazines.

Biological Activity

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.

in vivo

Gandotinib (LY2784544) effectively inhibits STAT5 phosphorylation in Ba/F3-JAK2V617F-GFP (green fluorescent protein) ascitic tumor cells (TED50=12.7 mg/kg) and significantly reduces (P<0.05) Ba/F3-JAK2V617F-GFP tumor burden in the JAK2V617F-induced MPN model (TED50=13.7 mg/kg, twice daily)[1].

target

wild-type JAK2

IC 50

JAK2: 3 nM (IC50); Tyk2: 44 nM (IC50); JAK3: 48 nM (IC50); FGFR2: 32 nM (IC50); FGFR3: 106 nM (IC50); Flt-4: 25 nM (IC50); KDR: 109 nM (IC50); FLT3: 4 nM (IC50); TRKB: 95 nM (IC50); ALK: 138 nM (IC50); MUSK: 147 nM (IC50); AURKA: 168 nM (IC50); MAP3K9: 299 nM (IC50)

LY 2784544Supplier

Shandong Yongxin Biotechnology Co., Ltd Gold
Tel
15866604075
Email
15195457346m@sina.cn
Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
J & K SCIENTIFIC LTD.
Tel
18210857532; 18210857532
Email
jkinfo@jkchemical.com
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Email
sales@BioChemBest.com
Jinan Trio PharmaTech Co., Ltd.
Tel
0531-88811783
Email
sales@trio-pharmatech.com
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