Product Details
Product Name:
Momelotinib |
CAS No.:
1056634-68-4 |
Min. Order:
1kg |
Purity:
99% |
Supply Ability:
100kg |
Release date:
2019/07/06 |
Product NUmber: :
WM.562 |
Momelotinib Basic information |
Description In vitro In vivo |
Product Name: |
Momelotinib |
Synonyms: |
momelotinib(JAK inhibitor)ORPHAN DRUG;CYT387, >=98%;Benzamide,N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-;CYT 11387;CYT 387;N-(Cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]benzamide;LM-1149;CYT 387(CYT 11387) |
CAS: |
1056634-68-4 |
MF: |
C23H22N6O2 |
MW: |
414.45978 |
EINECS: |
|
Product Categories: |
API;Inhibitors;Anti-cancer;Inhibitor |
Mol File: |
1056634-68-4.mol |
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Momelotinib Chemical Properties |
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Momelotinib Usage And Synthesis |
Description |
Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Phase 3. |
In vitro |
CYT387 inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 with IC50 of 1400 nM. Furthermore, 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, CYT387 has been shown to inhibit erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency with IC50 of 2μ-4 μM. A recent study shows that CYT387 inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Moreover, CYT387 induces apoptosis as a single agent and synergizes with the conventional anti-MM therapies bortezomib and melphalan in primary multiple myeloma (MM) cells. |
In vivo |
In a murine MPN model, CYT387 normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines. |
Company Profile Introduction
Established in 2014,Career Henan Chemical Co. is a manufacturerspecializing in the sale of fine chemicals.
Mainly deals in the sales of:
Pharmaceutical intermediates
OLED intermediates:
Pharmaceutical intermediates;
OLED intermediates;
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