NS-018 maleate

• CAT Number: I001371
• CAS Number: 1354799-87-3
• Molecular Formula: C25H24FN7O4
• Molecular Weight: 505.50
• Purity: ≥95%
• Target: Stem Cell/Wnt
• Solubility: DMSO ≥ 30 mg/mL
• Storage: Store at -20°C
• IUPAC Name: (Z)-but-2-enedioic acid;6-N-[(1S)-1-(4-fluorophenyl)ethyl]-4-(1-methylpyrazol-4-yl)-2-N-pyrazin-2-ylpyridine-2,6-diamine
• InChI: InChI=1S/C21H20FN7.C4H4O4/c1-14(15-3-5-18(22)6-4-15)26-19-9-16(17-11-25-29(2)13-17)10-20(27-19)28-21-12-23-7-8-24-21;5-3(6)1-2-4(7)8/h3-14H,1-2H3,(H2,24,26,27,28);1-2H,(H,5,6)(H,7,8)/b;2-1-/t14-;/m0./s1
• InChIKey: OVAGJAAQMBYZDS-FXSDFHGDSA-N
• SMILES: C[C@@H](C1=CC=C(C=C1)F)NC2=CC(=CC(=N2)NC3=NC=CN=C3)C4=CN(N=C4)C.C(=C\C(=O)O)\C(=O)O

NS-018 maleate（Cat No.:I001371）is an investigational compound being developed for its potential therapeutic effects in cancer treatment. It is a selective inhibitor of the protein kinase CK1α (casein kinase 1 alpha), which is involved in regulating cellular processes like cell division, circadian rhythm, and DNA repair. Overactivation of CK1α has been implicated in the development of various cancers. By targeting and inhibiting CK1α, NS-018 maleate aims to disrupt these processes, potentially reducing tumor growth and enhancing the response to other cancer treatments. The compound is currently undergoing preclinical studies to assess its efficacy and safety.

Reference

[1]. Kuroda J et al. NS-018, a selective JAK2 inhibitor, preferentially inhibits CFU-GM colony formation by bone marrow mononuclear cells from high-risk myelodysplastic syndrome patients. Leuk Res. 2014 May;38(5):619-24.

[2]. Nakaya Y et al. Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms. Blood Cancer J, 2011 Jul

[3]. Nakaya Y et al. Effect of NS-018, a selective JAK2V617F inhibitor, in a murine model of myelofibrosis. Blood Cancer J. 2014 Jan 10