Momelotinib
Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM, respectively. CYT387 shows much less activity against JAK3.
Product Specifications
CAS Number
1056634-68-4
Product Name Alternative
CYT387
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
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.html
Concentration
10mM
Purity
99.37
Solubility
DMSO : 10 mg/mL (ultrasonic; warming; adjust pH to 3 with HCl; heat to 60°C)
Smiles
O=C(C1=CC=C(C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2)C=C1)NCC#N
Molecular Formula
C23H22N6O2
Molecular Weight
414.46
Precautions
H302, H315, H319, H335
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]Monaghan KA, et al. The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells. Leukemia, 2011, 25 (12), 1891-1899.|[3]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.|[4]Kitajima S, et al.Overcoming Resistance to Dual Innate Immune and MEK Inhibition Downstream of KRAS.Cancer Cell. 2018 Sep 10;34 (3) :439-452.e6.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
JAK1; JAK2; JAK3
Citation 01
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.|Harvard Medical School LINCS LIBRARY
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