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Momelotinib
🥰Excellent
Catalog No. T1849Cas No. 1056634-68-4
Alias LM-1149, CYT387, CYT11387
Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells.
Momelotinib
🥰Excellent
Purity: 99.56%
Catalog No. T1849Alias LM-1149, CYT387, CYT11387Cas No. 1056634-68-4
Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $32 | In Stock | |
| 2 mg | $45 | In Stock | |
| 5 mg | $74 | In Stock | |
| 10 mg | $96 | In Stock | |
| 25 mg | $169 | In Stock | |
| 50 mg | $272 | In Stock | |
| 100 mg | $428 | In Stock | |
| 200 mg | $657 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $81 | In Stock |
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CitedSelect Batch
Purity:99.56%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells. |
| Targets&IC50 | JAK1:11 nM, JAK2:18 nM |
| In vitro | In a murine MPN model, CYT387 normalized blood cell density, white blood cell count and spleen size and restored physiological levels of inflammatory cytokines. |
| In vivo | In vitro, CYT387 inhibited IL-3-stimulated proliferation of parental Ba/F3 cells (IC50: 1400 nM). In addition, CYT387 inhibited the growth of red lineage colonies in JAK2V617F-positive PV patients in vitro with similar effect (IC50: 2-4 μM).CYT387 inhibited IGF-1- and IL-6-induced Ras/MAPK and PI3K/AKT signaling. In primary multiple myeloma cells, CYT387 alone or in combination with the MM therapeutic agents bortezomib and melphalan induced apoptosis.CYT387 was 9-fold more selective for JAK1 and JAK2 (IC50: 11 nM and 18 nM) than the JAK3 kinase (IC50: 155 nM).CYT387 also acted on cell lines with constitutive activation of JAK2 or MPL signaling. or MPL signaling cell lines, including Ba/F3-MPLW515L cells (IC50: 200 nM), CHRF-288-11 cells (IC50: 1 nM) and Ba/F3-TEL-JAK2 cells (IC50: 700 nM), and also inhibited cell proliferation. |
| Kinase Assay | Cell-free kinase activity assays: Glutathione-S-transferase (GST)-tagged JAK kinase domains expressed in insect cells are purified before use in a peptide substrate phosphorylation assay. Assays are carried out in 384-well optiplates using an Alphascreen Protein Tyrosine Kinase P100 detection kit and a PerkinElmer Fusion Alpha instrument. |
| Cell Research | Ba/F3 cells expressing JAK2V617F (Ba/F3-JAK2V617F) and MPLW515L (Ba/F3-MPLW515L) mutants, as well as CHRF-288-11 (JAK2T875N) and CMK (JAK3A572V) cells are used. The TEL/JAK2 and TEL/JAK3 fusions are generated and introduced into Ba/F3 murine cells. The TEL/JAK2- or TEL/JAK3-transfected cells are cultured in Dulbecco's modified Eagle's medium (DMEM) containing 10% fetal calf serum (FCS). Ba/F3 wild-type cells are cultured in RPMI containing 10% FCS supplemented with 5 ng/mL murine IL-3. Proliferation is measured using the Alamar Blue assay after incubating for 72 hours at 37 °C with 5% CO2 |
| Alias | LM-1149, CYT387, CYT11387 |
| Molecular Weight | 414.46 |
| Formula | C23H22N6O2 |
| Cas No. | 1056634-68-4 |
| Smiles | O=C(NCC#N)c1ccc(cc1)-c1ccnc(Nc2ccc(cc2)N2CCOCC2)n1 |
| Relative Density. | 1.292 g/cm3 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 69 mg/mL (166.5 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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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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