Nanatinostat

Nanatinostat (CHR-3996) is a potent, class I selective and orally active HDAC inhibitor with IC₅₀s of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. Nanatinostat has low activity against HDAC5 (IC₅₀ of 200 nM) and HDAC6 (IC₅₀ of 2100 nM). Nanatinostat induces apoptosis in myeloma cells. Nanatinostat has potent anticancer effects, such as myeloma, advanced solid tumours and colorectal cancer^[1][2][3]. IC50 & Target:IC50：8 nM ( HDAC)^[1] In Vitro:Nanatinostat (CHR-3996) (0.0001-1 μM; 48 hours) inhibits the proliferation of myeloma cell lines, with LC₅₀ values ranging from 30.3-97.6 nM in different cell lines^[2].
Nanatinostat (250-100 nM; 8-48 hours) induces apoptosis and increases the level of acetylated H3K9 in H929 and RPMI-8226 myeloma cell lines^[2].
Nanatinostat (0-200 nM; 24 hours) reduces the levels of IL-6 and VEGF secreted by bone marrow stromal cells in the co-culture system of bone marrow stromal cells and myeloma cells^[2].
Nanatinostat (250 nM and 100 nM; 48 hours) arrests the cell cycle at the G0/G1 phase in H929 and RPMI-8226 myeloma cell lines^[2].
In Vivo:Nanatinostat (50 mg/kg; orally administered; once daily; for 14 days) can almost completely inhibit tumor growth in the female CrTac:NCr-Fox1(nu) mouse HCT116 tumor xenograft model^[1].
Nanatinostat (25-50 mg/kg; orally administered; once daily; for 19 days) can significantly reduce tumor volume in a dose-dependent manner in the female BALB/c nude mouse LoVo human colon xenograft model^[1].
Nanatinostat (30 mg/kg; orally administered; once daily; for 28 days) can effectively inhibit tumor growth in the NOD/SCID IL2R gamma^null mouse myeloma model^[2].