产品
编 号:F527517
分子式:C18H20N2O3
分子量:312.36
产品类型
结构图
CAS No: 935881-37-1
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产品详情
生物活性:
AR-42 (HDAC-42; OSU-HDAC42) is a potent, orally bioavailable pan-HDAC inhibitor (IC50=16 nM). AR-42 induces growth inhibition, cell-cycle arrest, apoptosis, and activation of caspases-3/7. AR-42 promotes hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. AR-42 shows cytotoxicity against various human cancer cell lines.
体内研究:
AR-42 (10mg /kg;尾静脉注射;每周2次,连续3周)显著抑制肿瘤生长。Animal Model:Nude mice (HepG2 cell tumor xenograft model)
Dosage:10 mg/kg
Administration:Tail vein injection; twice a week for three weeks
Result:Significantly inhibited tumor growth.
体外研究:
Ar-42 (0.125-1 μM; 24 h) 抑制 P815、C2 和 BR 细胞生长的中位 IC50 分别为 0.65、0.30 和 0.23 μM。Ar-42 (0.5 μM; 24 h) 诱导 P815 细胞在 G1/G2 细胞周期阻滞。Ar-42 (0.13-1 μM; 24 h) 诱导 P815, C2, BR 细胞凋亡。Ar-42 (0.5-3 μM; 24 h) 诱导组蛋白 H3、H4 和 α-微管蛋白的超乙酰化。