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Momelotinib

Catalog No. T1849 CAS 1056634-68-4

Synonyms: CYT11387, CYT387, LM-1149

Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells.

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Momelotinib, CAS 1056634-68-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 32.00
2 mg	In stock	$ 45.00
5 mg	In stock	$ 74.00
10 mg	In stock	$ 96.00
25 mg	In stock	$ 169.00
50 mg	In stock	$ 272.00
100 mg	In stock	$ 428.00
200 mg	In stock	$ 657.00
1 mL * 10 mM (in DMSO)	In stock	$ 81.00

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Purity: 99.56%

Purity: 98.75%

Purity: 98%

Purity: 97.47%

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Description	Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells.
Targets&IC50	JAK2:18 nM, JAK1:11 nM
Kinase Assay	Cell-free kinase activity assays: Glutathione-S-transferase (GST)-tagged JAK kinase domains expressed in insect cells are purified before use in a peptide substrate phosphorylation assay. Assays are carried out in 384-well optiplates using an Alphascreen Protein Tyrosine Kinase P100 detection kit and a PerkinElmer Fusion Alpha instrument.
Cell Research	Ba/F3 cells expressing JAK2V617F (Ba/F3-JAK2V617F) and MPLW515L (Ba/F3-MPLW515L) mutants, as well as CHRF-288-11 (JAK2T875N) and CMK (JAK3A572V) cells are used. The TEL/JAK2 and TEL/JAK3 fusions are generated and introduced into Ba/F3 murine cells. The TEL/JAK2- or TEL/JAK3-transfected cells are cultured in Dulbecco's modified Eagle's medium (DMEM) containing 10% fetal calf serum (FCS). Ba/F3 wild-type cells are cultured in RPMI containing 10% FCS supplemented with 5 ng/mL murine IL-3. Proliferation is measured using the Alamar Blue assay after incubating for 72 hours at 37 °C with 5% CO2</sub(Only for Reference)

Synonyms	CYT11387, CYT387, LM-1149
Molecular Weight	414.46
Formula	C23H22N6O2
CAS No.	1056634-68-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 69 mg/mL (166.5 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Pardanani A, et al. Leukemia, 2009, 23(8), 1441-1445. 2. Monaghan KA, et al. Leukemia, 2011, 25(12), 1891-1899. 3. Tyner JW, et al. Blood, 2010, 115(25), 5232-5240. 4. Chen C, Lu M, Lin S, et al. The nuclear gene rpl18 regulates erythroid maturation via JAK2-STAT3 signaling in zebrafish model of Diamond–Blackfan anemia[J]. Cell Death & Disease. 2020, 11(2): 1-11. 5. Li M, Yu H. Identification of WP1066, an inhibitor of JAK2 and STAT3, as a Kv1. 3 potassium channel blocker[J]. . British Journal of Pharmacology. 2021

Citations

1. Li M, Yu H. Identification of WP1066, an inhibitor of JAK2 and STAT3, as a Kv1. 3 potassium channel blocker. British Journal of Pharmacology. 2021 Jul;178(13):2617-2631. doi: 10.1111/bph.15441. Epub 2021 May 20. 2. Chen C, Lu M, Lin S, et al. The nuclear gene rpl18 regulates erythroid maturation via JAK2-STAT3 signaling in zebrafish model of Diamond–Blackfan anemia. Cell Death & Disease. 2020, 11(2): 1-11

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library FDA-Approved Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Autophagy Compound Library

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Keywords

Momelotinib 1056634-68-4 Angiogenesis Apoptosis Autophagy Chromatin/Epigenetic JAK/STAT signaling Stem Cells JAK inhibit CYT11387 Janus kinase CYT 11387 Inhibitor CYT-387 CYT-11387 CYT387 LM 1149 CYT 387 LM-1149 LM1149 inhibitor

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