CYT 387(CAS#1056634-68-4)

Chemical Property:

Molecular Formula	C23H22N6O2
Molar Mass	414.46
Density	1.292
Solubility	DMSO ≥80mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
Appearance	Solid
pKa	10.94±0.46(Predicted)
Storage Condition	-20℃
MDL	MFCD16038899
Use	An inhibitor of JAK1 and JAK2.
In vitro study	CYT387 effectively and selectively acts on JAK1 and JAK2 with IC50 of 11 nM and 18 nM, respectively, which is 9 times more effective than the closely related JAK3 kinase (IC50 of 155 nM). In Vitro, CYT387 inhibits the proliferation of IL-3 stimulated parental Ba/F3 cells (Ba/F3-wt) with an IC50 of 1400 nM. Moreover, CYT387 acts on cell lines that constitutively activate JAK2 or MPL signaling, including Ba/F3-MPLW515L cells, CHRF-288-11 cells, and Ba/F3-TEL-JAK2 cells, and also inhibits cell proliferation, IC50 was 200 nM, 1 nM and 700 nM respectively. In addition, CYT387 had a similar effect in inhibiting erythroid colony growth of jak2v617f-positive PV patients in vitro, with an IC50 of 2 μ-4 μm. Recent studies have shown that CYT387 inhibits IL-6-and IGF-1-induced PI3K/AKT and Ras/MAPK signaling. Moreover, CYT387 alone and in combination with traditional anti-MM therapeutic drugs Bortezomib and Melphalan act on primary multiple myeloma (MM) cells to induce apoptosis.
In vivo study	CYT387 acts on the murine MPN model to normalize white blood cell count, blood cell density, spleen size, and restore physiological levels of inflammatory cytokines.

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CYT 387(CAS#1056634-68-4) Introduction

Momelotinib (CYT387) is an ATP competitive JAK1/JAK2 inhibitor with IC50 of 11 nM/18 nM, which is about 10 times more selective than JAK3.

pharmachologic effect
It is an ATP-competitive JAK1/JAK2 inhibitor with IC50s of 11 nM and 18 nM for JAK1 and JAK2, respectively, and selectivity for JAK3 is about 1/10 of that of JAK1 and JAK2, and can effectively inhibit the JAK-STAT signaling pathway, which is closely related to various biological processes such as cell proliferation, differentiation, and apoptosis, and can play a role in regulating immunity, anti-inflammatory, and anti-proliferation by inhibiting this pathway.345
Clinical application
It was approved by the FDA in September 2023 for the treatment of adult anemia with intermediate- or high-risk myelofibrosis (MF), including primary myelofibrosis or secondary myelofibrosis, i.e., polycythemia vera and essential thrombocythemia.
Adverse effects
The most common adverse reactions were thrombocytopenia, bleeding, bacterial infection, fatigue, dizziness, diarrhea and nausea.
Storage condition 5
Powder form can be stored at -20°C for 3 years and 4°C for 2 years.
After dissolving in solvents, it can be stored at -80°C for 6 months, and -20°C is recommended for 1 month.
use
It is used in cell experiments and animal experiments in scientific research to study JAK1/JAK2-related signaling pathways and disease mechanisms. Preclinical studies have shown potential for the treatment of diseases such as myelofibrosis, improving associated symptoms and improving patients’ quality of life134.
Synthesis method
It is usually prepared from 4-(4-morpholino)aniline and 4-chloropyrimidine as starting materials, and is prepared by multi-step reactions, such as condensation, substitution, and amidation.
CYT 387 is an important JAK inhibitor and has important implications in the treatment of myelofibrosis and other diseases, but its specific use should be carried out under the guidance of a physician.