Molecular Weight(MW): 469.94
Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2.
2 Customer Reviews
Relative expression of BCLXL, c-MYC, CCND1, MMP2 and VEGF in (A) HL60 cell line. Cells were treated with 1 µM of ruxolitinib, fedratinib, gandotinib or tofacitinib for 6 h. RE=1 for DMSO control. Asterix (*) denotes statistical significance (p<0.05). Error bars denotes±standard deviation. Each relative expression value was obtained from at least two biological experiments run in two technical repeats.
Eur J Pharmacol, 2015, 765:188-97. . Gandotinib (LY2784544) purchased from Selleck.
HEL cells were treated for 3 hours with the indicated concentrations of LY2784544. LY2784544 inhibits Jak2-V617F mediated signal transduction at submicromolar concentrations in intact cells.
M.Sc. Karoline Gaebler and Dr. Claude Haan of Université du Luxembour. Gandotinib (LY2784544) purchased from Selleck.
Purity & Quality Control
Choose Selective JAK Inhibitors
|Description||Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2.|
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.  Though biochemical assays do not reveal selectivity of LY2784544 for mutant JAK2V617F, LY2784544 shows higher selectivity for inhibition of JAK2-mediated signaling and induction of apoptosis in Ba/F3 cells expressing JAK2V617F than wild-type cells. 
|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. |
|In vitro||DMSO||94 mg/mL (200.02 mM)|
|Ethanol||9 mg/mL (19.15 mM)|
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01520220||Active, not recruiting||Myeloproliferative Neoplasms of|Polycythemia Vera|Essential Thrombocythemia|Myelofibrosis||Eli Lilly and Company||June 2012||Phase 1|
|NCT01594723||Active, not recruiting||Neoplasms, Hematologic||Eli Lilly and Company||May 2012||Phase 2|
|NCT01134120||Active, not recruiting||Myeloproliferative Disorders|Thrombocythemia, Essential|Polycythemia Vera|Primary Myelofibrosis||Eli Lilly and Company||April 2010||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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