Basic information Description In vitro In vivo Safety Related Supplier

ChemicalBook Product Catalog Biochemical Engineering Inhibitors protein tyrosine kinase Momelotinib

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Momelotinib

$ 2.00 /1kg

Min. Order1kg
Purity99%
Cas No1056634-68-4
Supply Ability100kg
Update time2019-07-06

career henan chemical co

career henan chemical co

6YR

China

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Chemical Properties

Product Name	Momelotinib
CAS No	1056634-68-4
EC-No
Min. Order	1kg
Purity	99%
Supply Ability	100kg
Release date	2019/07/06

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

Momelotinib Chemical Properties

density

1.292

Safety Information

MSDS Information

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.

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