Gandotinib (LY2784544)

Catalog No.S2179

Gandotinib (LY2784544) Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 320 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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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.

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Biological Activity

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.
Targets
JAK2 (V617F) [1] JAK2 [1] JAK2 [1]
(Cell-free assay)
FLT3 [2] JAK1 [2]
0.245 nM(Ki) 0.288 nM(Ki) 3 nM 4 nM 19.8 nM
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] 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. [2]

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]

Protocol

Solubility (25°C)

In vitro DMSO 94 mg/mL (200.02 mM)
Ethanol 9 mg/mL (19.15 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 469.94
Formula

C23H25ClFN7O

CAS No. 1229236-86-5
Storage powder
Synonyms N/A

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID