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Product Name:CYT387 (Mesylate) CAS:1056636-07-7
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| CYT387,MsOH salt Basic information |
Product Name: | CYT387,MsOH salt | Synonyms: | CYT387,MsOH salt;CYT387 (Mesylate);CYT 387 MESYLATE;CYT-387 MESYLATE;MOMELOTINIB MESYLATE;CS-1290;CYT387 mesylate
(CYT 387 mesylate;Momelotinib mesylate);MOMELOTINIB MESYLATE (CYT387 MESYLATE) | CAS: | 1056636-07-7 | MF: | C24H26N6O5S | MW: | 510.57 | EINECS: | | Product Categories: | | Mol File: | 1056636-07-7.mol | ![CYT387,MsOH salt Structure](CAS/20211123/GIF/1056636-07-7.gif) |
| CYT387,MsOH salt Chemical Properties |
storage temp. | Store at -20°C | solubility | Soluble in DMSO |
| CYT387,MsOH salt Usage And Synthesis |
Description | Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
JAK1|11 nM (IC50)|JAK2|18 nM (IC50)|JAK3|155 nM (IC50)
Momelotinib Mesylate is an inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3. Momelotinib inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 with IC50 of 1400 nM. Furthermore, Momelotinib also causes the inhibition of cell proliferation in cell lines constitutively activated by JAK2 or MPL signaling, including Ba/F3-MPLW515L cells, CHRF-288-11 cells and Ba/F3-TEL-JAK2 cells with IC50 of 200 nM, 1 nM and 700 nM, respectively. In addition, Momelotinib has been shown to inhibit erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency with IC50 of 2 μM-4 μM[1]. Momelotinib inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Moreover, Momelotinib 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 a murine MPN model, Momelotinib normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines[3]. | References | [1]. Pardanani A, et al. CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia, 2009, 23(8), 1441-1445.
[2]. Monaghan KA, et al. The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells. Leukemia, 2011, 25(12), 1891-1899.
[3]. Tyner JW, et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood, 2010, 115(25), 5232-5240. |
| CYT387,MsOH salt Preparation Products And Raw materials |
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