Momelotinib (sulfate)
Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM) .
Product Specifications
CAS Number
1056636-06-6
Product Name Alternative
CYT387 (sulfate salt)
UNSPSC
12352005
Target
Apoptosis; Autophagy; JAK
Type
Reference compound
Related Pathways
Apoptosis; Autophagy; Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/CYT387-sulfate-salt.html
Purity
99.91
Solubility
DMSO : 220 mg/mL (ultrasonic) |H2O : 100 mg/mL (ultrasonic)
Smiles
O=C(NCC#N)C(C=C1)=CC=C1C2=NC(NC(C=C3)=CC=C3N4CCOCC4)=NC=C2.O=S(O)(O)=O.O=S(O)(O)=O
Molecular Formula
C23H26N6O10S2
Molecular Weight
610.62
References & Citations
[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]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.|[3]Burns CJ, et al. Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs) . Bioorg Med Chem Lett. 2009 Oct 15;19 (20) :5887-92.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
JAK1; JAK2; JAK3
Citation 01
Harvard Medical School LINCS LIBRARY|BANGL J PHARMACOL. 2025 Apr 10;197 (5) :533.|bioRxiv. 2025 Oct 25.|Cancer Cell. 2018 Sep 10;34 (3) :439-452.e6. |Cancer Immunol Res. 2016 Jun;4 (6) :520-30.|Cancer Res. 2020 Jan 1;80 (1) :44-56. |Cell Death Dis. 2022 Dec 27;13 (12) :1075.|Cell Syst. 2018 Apr 25;6 (4) :424-443.e7.|Harvard Medical School LINCS LIBRARY|Immunol Invest. 2022 Aug;51 (6) :1582-1597.|Int J Biol Sci. 2022 Jan 1;18 (2) :585-598.|J Biotechnol. 2025 Mar:399:9-18.|J Enzyme Inhib Med Chem. 2025 Dec;40 (1) :2488127.|J Pineal Res. 2019 Apr;66 (3) :e12552.|Leukemia. 2012 Oct;26 (10) :2233-44.|Metabolism. 2025 Apr 4:156259.|Nat Commun. 2025 Jul 24;16 (1) :6777.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.
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