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Momelotinib (CYT387,CYT-387)

  Cat. No.:  DC3107   Featured
Chemical Structure
1056634-68-4
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Field of application
CYT387 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50 of 11 nM and 18 nM, respectively.
Cas No.: 1056634-68-4
Chemical Name: Momelotinib free base
Synonyms: N-(Cyanomethyl)-4-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)benzamide;CYT387;CYT-387;Momelotinib (CYT387);momelotinib(CYT-387);N-(Cyanomethyl)-4-(2-((4-morpholinophenyl)-amino)pyrimidin-4-yl)benzamide;N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]Benzamide;momelotinib;CYT 11387;LM-1149;Orange solid;CYT 387(CYT 11387);CYT387(momelotinib);momelotinib(JAK inhibitor)ORPHAN DRUG;CYT 387;N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide;6O01GMS00P;AK102858;N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide;N-(cyanomethyl)-4-(2-{[4-(morpholin-4-yl)phenyl]amino}pyrimidin-4-yl)be
SMILES: O1C([H])([H])C([H])([H])N(C2C([H])=C([H])C(=C([H])C=2[H])N([H])C2=NC([H])=C([H])C(C3C([H])=C([H])C(C(N([H])C([H])([H])C#N)=O)=C([H])C=3[H])=N2)C([H])([H])C1([H])[H]
Formula: C23H22N6O2
M.Wt: 414.46
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
In Vivo: In a murine MPN model, Momelotinib (CYT387) normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines[3].
In Vitro: Momelotinib (CYT387) inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 with IC50 of 1400 nM. Furthermore, Momelotinib (CYT387) 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 (CYT387) 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 (CYT387) inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Moreover, Momelotinib (CYT387) induces apoptosis as a single agent and synergizes with the conventional anti-MM therapies bortezomib and melphalan in primary multiple myeloma (MM) cells[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC7317 TG101209 TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations; TG101209 inhibit BRD4 activity with IC50 of 130 nM.
DC8309 Ruxolitinib Phosphate Ruxolitinib Phosphate is a potent and selective Janus kinase (JAK1, IC50 = 5.9 nM and JAK2, IC50 = 5.7 nM) inhibitor.
DC4230 Ruxolitinib (INCB018424) Ruxolitinib is a potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5 nM, respectively and is relatively less selective for JAK3 (IC50 = 322 nM).
DC3107 Momelotinib (CYT387,CYT-387) CYT387 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50 of 11 nM and 18 nM, respectively.
DC4175 BMS-911543 BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, approximately 350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively.
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