LM-1149
CYT387
CAS: 1056634-68-4
Molecular Formula: C23H22N6O2
LM-1149 - Names and Identifiers
LM-1149 - Physico-chemical Properties
| Molecular Formula | C23H22N6O2 |
| Molar Mass | 414.46 |
| Density | 1.292 |
| Solubility | DMSO ≥80mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
| Appearance | Solid |
| pKa | 10.94±0.46(Predicted) |
| Storage Condition | -20℃ |
| MDL | MFCD16038899 |
| Use | An inhibitor of JAK1 and JAK2. |
| In vitro study | CYT387 effectively and selectively acts on JAK1 and JAK2 with IC50 of 11 nM and 18 nM, respectively, which is 9 times more effective than the closely related JAK3 kinase (IC50 of 155 nM). In Vitro, CYT387 inhibits the proliferation of IL-3 stimulated parental Ba/F3 cells (Ba/F3-wt) with an IC50 of 1400 nM. Moreover, CYT387 acts on cell lines that constitutively activate JAK2 or MPL signaling, including Ba/F3-MPLW515L cells, CHRF-288-11 cells, and Ba/F3-TEL-JAK2 cells, and also inhibits cell proliferation, IC50 was 200 nM, 1 nM and 700 nM respectively. In addition, CYT387 had a similar effect in inhibiting erythroid colony growth of jak2v617f-positive PV patients in vitro, with an IC50 of 2 μ-4 μm. Recent studies have shown that CYT387 inhibits IL-6-and IGF-1-induced PI3K/AKT and Ras/MAPK signaling. Moreover, CYT387 alone and in combination with traditional anti-MM therapeutic drugs Bortezomib and Melphalan act on primary multiple myeloma (MM) cells to induce apoptosis. |
| In vivo study | CYT387 acts on the murine MPN model to normalize white blood cell count, blood cell density, spleen size, and restore physiological levels of inflammatory cytokines. |
LM-1149 - Introduction
Momelotinib (CYT387) is an ATP competitive JAK1/JAK2 inhibitor with IC50 of 11 nM/18 nM, which is about 10 times more selective than JAK3.
Last Update：2022-10-16 17:41:17
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Product Name: CYT387 Visit Supplier Webpage Request for quotationCAS: 1056634-68-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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