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CYT387 mesylate
CAS No. 1056636-07-7
CYT387 mesylate( CYT 387 mesylate | CYT-387 mesylate | Momelotinib mesylate )
Catalog No. M10261 CAS No. 1056636-07-7
A potent and selective JAK1/JAK2 inhibitor with IC50 of 11/18 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
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Biological Information
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Product NameCYT387 mesylate
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NoteResearch use only, not for human use.
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Brief DescriptionA potent and selective JAK1/JAK2 inhibitor with IC50 of 11/18 nM.
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DescriptionA potent and selective JAK1/JAK2 inhibitor with IC50 of 11/18 nM; shows significantly less activity against other kinases, including JAK3 (IC50=155 nM); inhibits JAK2V617F (JH1-JH2) withIC50 of 11 nM; inhibits growth of Ba/F3-JAK2V617F and HEL cells (IC50=1500 nM) or Ba/F3-MPLW515L cells (IC50=200 nM). Bone Cancer Phase 3 Clinical.
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In VitroMomelotinib 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. 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.
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In VivoIn a murine MPN model, Momelotinib normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines.
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SynonymsCYT 387 mesylate | CYT-387 mesylate | Momelotinib mesylate
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PathwayAngiogenesis
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TargetJAK
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RecptorJAK
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Research AreaCancer
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IndicationBone Cancer
Chemical Information
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CAS Number1056636-07-7
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Formula Weight510.5654
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Molecular FormulaC24H26N6O5S
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESCS(=O)(=O)O.C1COCCN1C2=CC=C(C=C2)NC3=NC=CC(=N3)C4=CC=C(C=C4)C(=O)NCC#N
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Chemical NameBenzamide, N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-, methanesulfonate (1:x)
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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PF-06651600
PF-06651600 is a novel potent, selective JAK3 inhibitor with IC50 of 0.346 nM, displays >1,000-fold selectivity over JAK1 and JAK2; inhibits Th1 and Th17 cell differentiation and function, reduces disease pathology in rat adjuvant-induced arthritis as well as in mouse experimental autoimmune encephalomyelitis models; selectively targets γc cytokine pathways while preserving JAK1-dependent anti-inflammatory signaling such as the IL-10 suppressive functions following LPS treatment in macrophages and the suppression of TNFα and IL-1β production in IL-27-primed macrophages.Rheumatoid ArthritisPhase 2 Clinical
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CEP-33779
CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
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Tofacitinib
Tofacitinib (CP-690550) is a potent, specific, orally active inhibitor of JAK3 with IC50 of 1 nM in cell-free assays; displays 20- to 100-fold less potency for JAK2 and JAK1 (IC50=20 nM and 112 nM, respectively).
