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CYT387 CAS: 1056634-68-4

Category: Inhibitors
Product Name: CYT387
Cat No: I000293
CAS No: 1056634-68-4
Synonyms: N-(cyanomethyl)-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide
Molecular Formula: C23H22N6O2
Molecular Weight: 414.5
SMILES: O=C(NCC#N)C(C=C1)=CC=C1C2=NC(NC(C=C3)=CC=C3N4CCOCC4)=NC=C2
InChI: None
InChIKey: ZVHNDZWQTBEVRY-UHFFFAOYSA-N
Solubility: DMSO: ≥ 72.5 mg/mL
Target: JAK
IC50: 11 nM/18 nM(JAK1/JAK2) [1]
Storage: powder
CAS 1056634-68-4,CYT387
  • Description

CYT387(momelotinib) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3.
IC50 value: 11 nM/18 nM(JAK1/JAK2) [1]
Target: JAK1/JAK2
in vitro: CYT387 inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 with IC50 of 1400 nM. Furthermore, CYT387 also causes the inhibition of cell proliferation in cell lines constitutively activated by JAK2 or MPL signaling, including Ba/F3-MPLW515L cells, CHRF-288-11 cells and Ba/F3-TEL-JAK2 cells with IC50 of 200 nM, 1 nM and 700 nM, respectively. In addition, CYT387 has been shown to inhibit erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency with IC50 of 2μ-4 μM [1]. A recent study shows that CYT387 inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Moreover, CYT387 induces apoptosis as a single agent and synergizes with the conventional anti-MM therapies bortezomib and melphalan in primary multiple myeloma (MM) cells [2].
in vivo: In a murine MPN model, CYT387 normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines [3].

  • Spec

Appearance:Yellow solid powder
Purity: > 98%

  • References


1:Enhanced Antitumor Activity of Cetuximab in Combination with the Jak Inhibitor CYT387 against Non-Small-Cell Lung Cancer with Various Genotypes. Hu Y, Dong XZ, Liu X, Liu P, Chen YB.Mol Pharm. 2016 Feb 1;13(2):689-97. doi: 10.1021/acs.molpharmaceut.5b00927. Epub 2015 Dec 29. PMID: 26685983
2:P-glycoprotein (MDR1/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) restrict brain accumulation of the JAK1/2 inhibitor, CYT387. Durmus S, Xu N, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.Pharmacol Res. 2013 Oct;76:9-16. doi: 10.1016/j.phrs.2013.06.009. Epub 2013 Jul 1. PMID: 23827160
3:Safety and efficacy of CYT387, a JAK1 and JAK2 inhibitor, in myelofibrosis. Pardanani A, Laborde RR, Lasho TL, Finke C, Begna K, Al-Kali A, Hogan WJ, Litzow MR, Leontovich A, Kowalski M, Tefferi A.Leukemia. 2013 Jun;27(6):1322-7. doi: 10.1038/leu.2013.71. Epub 2013 Mar 5. PMID: 23459451 Free PMC Article
4:Liquid chromatography-tandem mass spectrometric assay for the JAK2 inhibitor CYT387 in plasma. Sparidans RW, Durmus S, Xu N, Schinkel AH, Schellens JH, Beijnen JH.J Chromatogr B Analyt Technol Biomed Life Sci. 2012 May 1;895-896:174-7. doi: 10.1016/j.jchromb.2012.03.021. Epub 2012 Mar 23. PMID: 22476054
5:The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells. Monaghan KA, Khong T, Burns CJ, Spencer A.Leukemia. 2011 Dec;25(12):1891-9. doi: 10.1038/leu.2011.175. Epub 2011 Jul 26. PMID: 21788946
6:CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Tyner JW, Bumm TG, Deininger J, Wood L, Aichberger KJ, Loriaux MM, Druker BJ, Burns CJ, Fantino E, Deininger MW.Blood. 2010 Jun 24;115(25):5232-40. doi: 10.1182/blood-2009-05-223727. Epub 2010 Apr 12. PMID: 20385788 Free PMC Article
7: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. Pardanani A, Lasho T, Smith G, Burns CJ, Fantino E, Tefferi A.Leukemia. 2009 Aug;23(8):1441-5. doi: 10.1038/leu.2009.50. Epub 2009 Mar 19. PMID: 19295546


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