Home JAK/STAT JAK inhibitor Gandotinib (LY2784544) For research use only.

Gandotinib (LY2784544)

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

Gandotinib (LY2784544) Chemical Structure

CAS No. 1229236-86-5

Purity & Quality Control

Gandotinib (LY2784544) Related Products

Signaling Pathway

JAK Signaling Pathways

JAK Signaling Pathway

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01520220 Completed
Myeloproliferative Neoplasms of|Polycythemia Vera|Essential Thrombocythemia|Myelofibrosis
Eli Lilly and Company
 June 11 2012 Phase 1
NCT01594723 Active not recruiting
Neoplasms Hematologic
Eli Lilly and Company
 May 22 2012 Phase 2
NCT01577355 Completed
Healthy Male Volunteers
Eli Lilly and Company
 April 2012 Phase 1
NCT01134120 Completed
Myeloproliferative Disorders|Thrombocythemia Essential|Polycythemia Vera|Primary Myelofibrosis
Eli Lilly and Company
 April 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 469.94 Formula

C23H25ClFN7O
CAS No. 1229236-86-5 SDF Download Gandotinib (LY2784544) SDF
Smiles CC1=CC(=NN1)NC2=NN3C(=C(N=C3C(=C2)CN4CCOCC4)C)CC5=C(C=C(C=C5)Cl)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 94 mg/mL ( (200.02 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 9 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Gandotinib (LY2784544) | Gandotinib (LY2784544) supplier | purchase Gandotinib (LY2784544) | Gandotinib (LY2784544) cost | Gandotinib (LY2784544) manufacturer | order Gandotinib (LY2784544) | Gandotinib (LY2784544) distributor