CYT387,MsOH salt
- Product NameCYT387,MsOH salt
- CAS1056636-07-7
- CBNumberCB42627744
- MFC24H26N6O5S
- MW510.57
- MDL NumberMFCD18251579
- MOL File1056636-07-7.mol
Chemical Properties
storage temp. | Store at -20°C |
solubility | Soluble in DMSO |
CYT387,MsOH salt Price
Product number | Packaging | Price | Product description | Buy |
---|---|---|---|---|
Biorbyt Ltd orb611828 | 10mg | $238 | CYT387 mesylate |
Buy |
Biorbyt Ltd orb611828 | 50mg | $508.3 | CYT387 mesylate |
Buy |
Biorbyt Ltd orb611828 | 100mg | $657.9 | CYT387 mesylate |
Buy |
Crysdot CD31004689 | 5mg | $60 | CYT387Mesylate 98+% |
Buy |
DC Chemicals DC24066 | 10mg | $84 | CYT387mesylate >98% |
Buy |
CYT387,MsOH salt Chemical Properties,Usage,Production
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.
Preparation Products And Raw materials
CYT387,MsOH salt Suppliers
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