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CAS No. 1229236-86-5
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.
Selleck's Gandotinib (LY2784544) has been cited by 16 publications
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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.
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.
(F) SGC-7901 cells were treated with JAK2 specific inhibitor of LY2784544 (5 nM) for 1 h, and then p-JAK2 expressions were measured using western blot analysis. SGC-7901 cells were pretreated with LY2784544 (5 nM) for 1 h, followed by APG (50 mM) incubation for another 24 h. Following, (G) The cell viability and (H) apoptosis were calculated. ***P < 0.001 versus the Con group. ###P < 0.001 versus the IL-6 group; þþþP < 0.001 versus the IL-6/APG group. Data are represented as mean ± SEM (n = 8).
Biochem Biophys Res Commun, 2018, 498(1):164-170. Gandotinib (LY2784544) purchased from Selleck.
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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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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01520220||Completed||Drug: LY2784544||Myeloproliferative Neoplasms of|Polycythemia Vera|Essential Thrombocythemia|Myelofibrosis||Eli Lilly and Company||June 11 2012||Phase 1|
|NCT01594723||Active not recruiting||Drug: 120 mg LY2784544||Neoplasms Hematologic||Eli Lilly and Company||May 22 2012||Phase 2|
|NCT01577355||Completed||Radiation: Drug||Healthy Male Volunteers||Eli Lilly and Company||April 2012||Phase 1|
|NCT01134120||Completed||Drug: LY2784544||Myeloproliferative Disorders|Thrombocythemia Essential|Polycythemia Vera|Primary Myelofibrosis||Eli Lilly and Company||April 2010||Phase 1|
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