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编 号:F282844
分子式:C28H38N8O5
分子量:566.65
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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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生物活性:
HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies.

体内研究:
HDACs/mTOR Inhibitor 1 (Compound 12l) (10 or 20 mg/kg, 尾静脉注射) 在 MV4-11 和 MM1S 移植瘤 NOD/SCID 小鼠模型中抑制肿瘤生长,且没有明显毒性。Animal Model:MV4-11 xenograft NOD/SCID mouse model
Dosage:10 mg/kg
Administration:Intravenous injection (i.v.), every two days (Q2D)×6
Result:The TGI (tumor growth inhibitory rate) was 53.1%.

体外研究:
HDACs/mTOR Inhibitor 1 (Compound 12l) 抑制白血病细胞增殖,对 MV4-11, OCI-AML2, OCI-AML3IC 的50s 分别为 4.05, 9.01, 9.98 μM。HDACs/mTOR Inhibitor 1 (0-10 μM, 6 h or 24 h) 在 MV4-11 细胞中下调 p-ERK 水平,上调 Ac-H3 水平。HDACs/mTOR Inhibitor 1 (10 to 1000 nM, 48 h) 减少 S 期 MV4-11 细胞细胞并增加 G0/G1 期细胞的百分比。
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