LY2784544

• Catalog No.: S2179
• CAS Number: 1229236-86-5
• M. F.: C23H25ClFN7O
• M. W.: 469.9423032
• Storage: -20°C

SYNONYMS

• 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

DATABASE IDS

• CAS Number: 1229236-86-5

PROPERTIES

• Target: JAK
• Salt Data: Free Base
• Storage Condition: -20°C

DETAILS

Description (English)

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.

References

• References: [1] Ma L, et al. 53rd ASH Annual Meeting and Exposition, 2011, Abstract 4087.

REFERENCES

• Ma L, et al. 53rd ASH Annual Meeting and Exposition, 2011, Abstract 4087.