Momelotinib mesylate (CYT387) | JAK1/2 inhibitor

Chemical Structure : CYT387 mesylate

CYT387 mesylate (CYT-387 mesylate, Momelotinib mesylate)

Catalog No.: PC-42753Not For Human Use, Lab Use Only.

Momelotinib mesylate (CYT387 mesylate) is a potent and selective JAK1/JAK2 inhibitor with IC50 of 11/18 nM.

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Biological Activity

Momelotinib mesylate (CYT387 mesylate) is a potent and selective JAK1/JAK2 inhibitor with IC50 of 11/18 nM.
Momelotinib mesylate (CYT387 mesylate) shows significantly less activity against other kinases, including JAK3 (IC50=155 nM).
Momelotinib mesylate (CYT387 mesylate) inhibits JAK2V617F (JH1-JH2) withIC50 of 11 nM.
Momelotinib mesylate (CYT387 mesylate) inhibits growth of Ba/F3-JAK2V617F and HEL cells (IC50=1500 nM) or Ba/F3-MPLW515L cells (IC50=200 nM).

Physicochemical Properties

M.Wt	510.5654
Formula	C24H26N6O5S
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Benzamide, N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-, methanesulfonate (1:x)

References

1. Pardanani A, et al. Leukemia. 2009 Aug;23(8):1441-5.

2. Burns CJ, et al. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5887-92.

3. Tyner JW, et al. Blood. 2010 Jun 24;115(25):5232-40.

CYT387 mesylate (CYT-387 mesylate, Momelotinib mesylate)

Biological Activity

Physicochemical Properties

References

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