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別品名 BMS-708163
別包装 あり
分子量 520.89
CAS RN® 1146699-66-2
構造 C20H17ClF4N4O4S
使用目的 BMS-708163 is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; BMS-708163 also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM.IC50 & Target: IC50: 0.27 nM (γ-secretase, Aβ42), 0.30 nM (γ-secretase, Aβ40), 20 μM (CYP2C19)[1], 0.84 nM (NICD)[2]In Vitro: BMS-708163 exhibits weaker potency for inhibition of Notch processing, IC50=58±23 nM, as compared to its inhibition potency for APP cleavage[1]. BMS-708163 (10?μM) 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. BMS-708163 induces apoptosis and enhances cell cycle arrest at the G1 phase in PC9/AB2 cells. BMS-708163 treatment effectively downregulates the expression of Notch1, HES1, PI3K and Akt in PC9/AB2 cells[3].In Vivo: 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[1]. 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 BMS-708163 plus gefitinib, there are a marked increase in caspase 3 expression and a reduction in Ki-67 staining[3].
参考文献 J Alzheimers Dis. 2012;28(4):809-22.
EMBO J. 2012 May 16;31(10):2261-74.
[注意事項] [溶解度表記について]MCH社のWeb及びデータシート等で溶解度が「<1 mg/ml」のように記載されている場合、その化合物はその溶媒に、溶けないまたはわずかに溶けることを意味しています。(この場合、1mg/ml以下の濃度では試験していません。)
「>90mg/mL」のように記載されている場合、その化合物はその溶媒に90mg/ml で溶けたことを示しています。(ただし、最大でどのくらい溶けるかは試験していません。)


メーカー 品番 包装
MCH HY-50845 10 MG
希望販売価格 ¥85,000


当社在庫 なし
納期目安 約10日
保存温度 -20℃




メーカー名 MedChemexpress Co., limited
略号 MCH