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Momelotinib Mesylate

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Momelotinib Mesylate

Catalog No. T15037Cas No. 1056636-07-7

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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Pack Size	Price	Availability	Quantity
25 mg	$1,520	1-2 weeks

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Product Introduction

Bioactivity

Description	Momelotinib Mesylate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
Targets&IC50	JAK3:155 nM, JAK2:18 nM, JAK1:11 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].
Alias	CYT387 (Mesylate)

Chemical Properties

Molecular Weight	510.57
Formula	C24H26N6O5S
Cas No.	1056636-07-7

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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