LY2784544 also inhibits IL-3-activated wild type JAK2 with IC50 of 2.26 ¦ÌM. Similarly in the proliferation assay, LY2784544 shows antiproliferation activity in JAK2 V617F-driven cells with IC50 of 68 nM, compared to 1.36 ¦ÌM in wild type JAK2-driven cells and 0.94 ¦ÌM in JAK3-driven cells.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.

June 21, 2017

prudect name : LY2784544 also inhibits IL-3-activated wild type JAK2 with IC50 of 2.26 ¦ÌM. Similarly in the proliferation assay, LY2784544 shows antiproliferation activity in JAK2 V617F-driven cells with IC50 of 68 nM, compared to 1.36 ¦ÌM in wild type JAK2-driven cells and 0.94 ¦ÌM in JAK3-driven cells.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.
LY2784544

Synonyms: CAS NO: 1229236-86-5Molecular Formula: C23H25ClFN7OMolecular Weight: 469.94Purity: 98% minSolubility: In DMSOStorage: −20°C


web site: www.medchemexpress.com

References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18524244