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CYT387JAK-1/-2 inhibitor,ATP competitive

CYT387

Catalog No. A4143
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $80.00 In stock
10mg $110.00 In stock
50mg $300.00 In stock
200mg $770.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

CYT387

Related Biological Data

CYT387

Related Biological Data

CYT387

Biological Activity

Description Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3.
Targets JAK1 JAK2 JAK3      
IC50 11 nM 18 nM 155 nM      

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Chemical Properties

Cas No. 1056634-68-4 SDF Download SDF
Synonyms Cyt-387,MOMELOTINIB,CYT 387,CYT 11387
Chemical Name N-(cyanomethyl)-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide
Canonical SMILES C1COCCN1C2=CC=C(C=C2)NC3=NC=CC(=N3)C4=CC=C(C=C4)C(=O)NCC#N
Formula C23H22N6O2 M.Wt 414.46
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Background

CYT387, an aminopyrimidine derivative discovered by high-throughput enzyme and cell-based screening along with the optimization using structure-guided medicinal chemistry, is a potent and selective inhibitor of janus kinase 1 (JAK1), janus kinase 2 (JAK2) and tyrosine kinase 2 (TYK2) with values of 50% inhibition concentration IC50 of 11 nM, 18 nM, 155 nM and 17 nM respectively. Recent studies have revealed that CYT387, at low nanomolar concentrations ranging between 500 and 1500 nM, is able to inhibit JAK2 signaling pathway, suppress proliferation and induce apoptosis in JAK2-dependent hematopoietic cell lines with non-hematopoietic cell lines intact.

Reference

Tyner JW, Bumm TG, Deininger J, Wood L, Aichberger KJ, Loriaux MM, Druker BJ, Burns CJ, Fantino E, Deininger MW. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood. 2010;115(25):5232-5240.