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Avagacestat
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Avagacestat
CAS No. : 1146699-66-2
MCE 站:Avagacestat
产品活性:Avagacestat (BMS-708163) 是有效的 γ-secretase 抑制剂,抑制 Aβ42 和 Aβ40 的产生,IC50 值分别为 0.27 nM 和 0.30 nM;BMS-708163 同时抑制 Notch 胞内结构域 (NICD) 和 CYP2C19,IC50 值分别为 0.84 nM 和 20 μM。
研究领域:Neuronal Signaling | Stem Cell/Wnt
作用靶点:γ-secretase | Notch
In Vitro: Avagacestat (BMS-708163) exhibits weaker potency for inhibition of Notch processing, IC50=58±23 nM, as compared to its inhibition potency for APP cleavage. Avagacestat (BMS-708163) (10??M) combined with gefitinib significantly attenuates the colony growth of PC9/AB2 cells, increases the expression of active caspase 3 and PARP and reduces the expression of Ki-67 in PC9/AB2 cells. Avagacestat (BMS-708163) induces apoptosis and enhances cell cycle arrest at the G1 phase in PC9/AB2 cells. Avagacestat (BMS-708163) treatment effectively downregulates the expression of Notch1, HES1, PI3K and Akt in PC9/AB2 cells.
In Vivo: Avagacestat (BMS-708163) significantly reduces both plasma and brain Aβ40 levels relative to control at 10 and 100 mg/kg for the entire dosing interval, demonstrates significant Aβ40 lowering for 8 h after an oral dose of 1 mg/kg, and significantly lowers CSF Aβ40 levels in rats, when measured 5 h after single oral doses ranging from 3 to 100 mg/kg. Avagacestat (BMS-708163) (10?mg/kg) monotherapy has a minor inhibitory effect on PC9/AB2 tumor growth compared with gefitinib alone. BMS-708163 monotherapy results in a slight increase in caspase 3 expression as well as a mild decrease in Ki-67 expression in vivo. In the xenograft lung cancer samples treated with Avagacestat (BMS-708163) plus gefitinib, there are a marked increase in caspase 3 expression and a reduction in Ki-67 staining.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Neuronal Signaling Compound Library | Stem Cell Signaling Compound Library | Wnt/Hedgehog/Notch Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | DAPT | Valproic acid | YO-01027 | LY-411575 | Compound E | CB-103 | Tangeretin | Jagged-1 (188-204) (TFA) | E 2012 | IMR-1 | L-685458 | Semagacestat | Carvacrol | RBPJ Inhibitor-1 | JI051 | Bruceine D | NGP555 | BMS 299897 | ZLDI-8 | Psoralidin | Sulindac sulfide | Begacestat | Z-Ile-Leu-aldehyde | gamma-secretase modulator 3 | BMS 433796 | SAHM1
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