Identification | Back Directory | [Name]
LY 2784544 | [CAS]
1229236-86-5 | [Synonyms]
CS-13 LY2874544 Tucatinib LY 2784544 LY2784544/LY-2784544 LY2784544(gandotinib) Gandotinib (LY2784544) 3-(4-Chloro-2-fluorobenzyl)-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholinomethyl)imidazo[ 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-fluorobenzyl)-2-Methyl-N-(3-Methyl-1H-pyrazol-5-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 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)- 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 | [Molecular Formula]
C23H25ClFN7O | [MDL Number]
MFCD20482143 | [MOL File]
1229236-86-5.mol | [Molecular Weight]
469.94 |
Chemical Properties | Back Directory | [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 |
Hazard Information | Back Directory | [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 activeATP-competitivepotent and JAK2-selective janus tyrosine kinase inhibitor (IC50/[ATP] = 2.52 nM/5 μM/JAK219.8 nM/20 μM/JAK148.0 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 activitybut not 11 other GPRs. | [target]
wild-type JAK2 |
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