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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
😃Good
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 Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $1,520 | 1-2 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| 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]. |
| Alias | CYT387 (Mesylate) |
| Molecular Weight | 510.57 |
| Formula | C24H26N6O5S |
| Cas No. | 1056636-07-7 |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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