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Momelotinib Mesylate

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Catalog No. T15037Cas No. 1056636-07-7
Alias CYT387 (Mesylate)

Momelotinib Mesylate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.

Momelotinib Mesylate
Other Forms of Momelotinib Mesylate:

Momelotinib Mesylate

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Catalog No. T15037Alias CYT387 (Mesylate)Cas No. 1056636-07-7
Momelotinib Mesylate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$1,5201-2 weeks1-2 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
Momelotinib Mesylate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
Targets&IC50
JAK1:11 nM, JAK2:18 nM, JAK3:155 nM
In vitro
Momelotinib inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 (IC50: 1400 nM) and it also inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Momelotinib inhibits erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency (IC50: 2 μM-4 μM) [1]. Momelotinib causes the inhibition of cell proliferation in cell lines constitutively activated by JAK2 or MPL signaling, including Ba/F3-MPLW515L cells, Ba/F3-TEL-JAK2 cells and CHRF-288-11 cells (IC50: 200 nM, 1 nM and 700 nM, respectively) and it also induces apoptosis as a single agent and synergizes with the conventional anti-MM therapies bortezomib and melphalan in primary multiple myeloma (MM) cells [2].
In vivo
Momelotinib normalizes white cell counts, spleen size, hematocrit, in a murine MPN model. It also restores physiologic levels of inflammatory cytokines [3].
SynonymsCYT387 (Mesylate)
Chemical Properties
Molecular Weight510.57
FormulaC24H26N6O5S
Cas No.1056636-07-7
SmilesCS(O)(=O)=O.O=C(NCC#N)c1ccc(cc1)-c1ccnc(Nc2ccc(cc2)N2CCOCC2)n1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

Momelotinib MesylateJAK3JAK2JAK1CYT-387CYT387CYT 387
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