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Momelotinib Mesylate

Catalog No. T15037 CAS 1056636-07-7

Synonyms: CYT387 (Mesylate)

Momelotinib Mesylate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.

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Momelotinib Mesylate, CAS 1056636-07-7

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25 mg	6-8 weeks	$ 1,520.00

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Description	Momelotinib Mesylate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
Targets&IC50	JAK2:18 nM, JAK1:11 nM, JAK3:155 nM
In vitro	Momelotinib inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 (IC50: 1400 nM) and it also inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Momelotinib inhibits erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency (IC50: 2 μM-4 μM) [1]. Momelotinib causes the inhibition of cell proliferation in cell lines constitutively activated by JAK2 or MPL signaling, including Ba/F3-MPLW515L cells, Ba/F3-TEL-JAK2 cells and CHRF-288-11 cells (IC50: 200 nM, 1 nM and 700 nM, respectively) and it also 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	Momelotinib normalizes white cell counts, spleen size, hematocrit, in a murine MPN model. It also restores physiologic levels of inflammatory cytokines [3].

Synonyms	CYT387 (Mesylate)
Molecular Weight	510.57
Formula	C24H26N6O5S
CAS No.	1056636-07-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Pardanani A, et al. CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia, 2009, 23(8), 1441-1445. 2. Monaghan KA, et al. The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells. Leukemia, 2011, 25(12), 1891-1899. 3. Tyner JW, et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood, 2010, 115(25), 5232-5240.

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Keywords

Momelotinib Mesylate 1056636-07-7 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells JAK CYT387 (Mesylate) CYT387 CYT 387 CYT-387 inhibitor inhibit

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