Gandotinib (LY2784544)

Catalog No.S2179

For research use only.

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.

Gandotinib (LY2784544) Chemical Structure

CAS No. 1229236-86-5

Selleck's Gandotinib (LY2784544) has been cited by 20 publications

Purity & Quality Control

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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] Click to View More Targets
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 (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 469.94
Formula

C23H25ClFN7O

CAS No. 1229236-86-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=NN1)NC2=NN3C(=C(N=C3C(=C2)CN4CCOCC4)C)CC5=C(C=C(C=C5)Cl)F

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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.

Handling Instructions

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