Substance
ID:73710
Names and Identifiers
IUPAC name
N-{3-[(4-chloro-2-fluorophenyl)methyl]-2-methyl-8-(morpholin-4-ylmethyl)imidazo[1,2-b]pyridazin-6-yl}-3-methyl-1H-pyrazol-5-amine
IUPAC Traditional name
N-{3-[(4-chloro-2-fluorophenyl)methyl]-2-methyl-8-(morpholin-4-ylmethyl)imidazo[1,2-b]pyridazin-6-yl}-5-methyl-2H-pyrazol-3-amine
Synonyms
LY2784544
Registration numbers
CAS Number
Properties
Safety Information
Storage Condition
-20°C
Pharmacology Properties
Target
JAK
Product Information
Salt Data
Free Base
Molecule Details
Research Area
Description
Myeloproliferative disorders
Biological Activity
Description
LY2784544 is selective to V617F mutant JAK2 with IC50 of 55 nM in Ba/F3 cells.
Targets
JAK2 V617F mutant
IC50
55 nM [1]
In Vitro
LY2784544 also inhibits IL-3-activated wild type JAK2 with IC50 of 2.26 μM. Similarly in the proliferation assay, LY2784544 shows antiproliferation activity in JAK2 V617F-driven cells with IC50 of 68 nM, compared to 1.36 μM in wild type JAK2-driven cells and 0.94 μM in JAK3-driven cells. [1]
In Vivo
LY2784544 significantly inhibits STAT5 phosphorylation in Ba/F3-JAK2 V617F-GFP xenografts with a Threshold Effective Dose 50 (TED50) of 12.7 mg/kg. LY2784544 also reduces Ba/F3-JAK2 V617F-GFP tumor burden in the JAK2 V617F-induced MPN model with a TED50 of 13.7 mg/kg after oral treatment. LY2784544 has no effect on CD71/Ter119 positive erythroid progenitors in spleens of SCID mice after oral treatment. [1]
Clinical Trials
Currently in Phase I clinical trial in patients with JAK2 V617F-positive myeloproliferative disorders.
Features
Molecular Spectra
No Data Available
Click here to submit data
References
• Ma L, et al. 53rd ASH Annual Meeting and Exposition, 2011, Abstract 4087.