Momelotinib (sulfate)
Product Specifications
UNSPSC Description
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).
Target Antigen
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
98.06
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 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.Harvard Medical School LINCS LIBRARY|BANGL J PHARMACOL. 2023 Dec 17.|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. 2021 Oct 27;1-16.|Int J Biol Sci. 2022 Jan 1;18(2):585-598.|Int J Biol Sci. 2022; 18(2): 585-598.|J Pineal Res. 2019 Apr;66(3):e12552.|Leukemia. 2012 Oct;26(10):2233-44.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-10962/Momelotinib-sulfate-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-10962/Momelotinib-sulfate-SDS-MedChemExpress.pdf
Clinical Information
Phase 3
CAS Number
1056636-06-6
Available Sizes
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