Momelotinib NEW
| Price | $32 | $45 | $74 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Momelotinib | CAS No.: 1056634-68-4 |
| Purity: 99.56% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Momelotinib |
| 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. |
| 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 |
| 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. |
| 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. |
| 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) |
| Keywords | inhibit | JAK | Janus kinase | CYT 11387 | Inhibitor | CYT-387 | CYT-11387 | Autophagy | Apoptosis | LM 1149 | Momelotinib | CYT 387 | LM1149 |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Tributyrin | Curcumin | Paeonol | Naringin | Gefitinib |
| Related Compound Libraries | Bioactive Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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