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编 号:F281988
分子式:C24H21N3O4
分子量:415.44
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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生物活性:
J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1.

体内研究:
J22352 (10 mg/kg;在雄性裸鼠中每天腹膜内给药,持续 14 天) 导致 >80% 的肿瘤生长抑制 (TGI) 率。J22352 在小鼠中具有良好的耐受性。Animal Model:Male nude mice (BALB/cAnN.Cg-Foxnlnu/CrlNarl, 4-6 weeks old)
Dosage:10?mg/kg
Administration:Given i.p.; per day for 14 days
Result:Marked anti-tumor effects and well tolerated in mice.

体外研究:
J22352 (0.1 -20 μM;72 小时) 以剂量依赖性方式降低 U87MG 细胞活力。 J22352 (10 μM;24 小时) 剂量依赖性降低 HDAC6 蛋白丰度。
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