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Cyt387 CAS NO.1056634-68-4
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- Min.Order: 100 Gram
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≥98.0%(100-500)Gram≥98.0%(1000-5000)Gram
- Product Details
Keywords
- Cyt387
- CYT 11387;CYT 387;N-(Cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]benzamide;LM-1149;CYT 387(CYT 11387);N-(cyanoMethyl)-4-(2-(4-Morpholin-4-ylphenylaMino)pyriMidin-4-yl)benzaMide;Mo
- 1056634-68-4
Quick Details
- ProName: Cyt387
- CasNo: 1056634-68-4
- Molecular Formula: C23H22N6O2
- Appearance: close to white solid
- Application: CAS：1056634-68-4； CYT 11387;CYT 387;N...
- DeliveryTime: 3 months
- PackAge: 100g,500g,1kg,25kg
- Port: shang hai
- ProductionCapacity: 100 Gram/Month
- Purity: 98%
- Storage: Dry seal
- Transportation: shipping
- LimitNum: 100 Gram
Superiority
We are committed to provide excellence in researching, manufacturing and drug discovery process.
Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.
Details
CYT387(momelotinib) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3.
IC50 value: 11 nM/18 nM(JAK1/JAK2) [1]
Target: JAK1/JAK2
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 [1]. 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 [2].
in vivo: In a murine MPN model, CYT387 normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines [3].