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  2. Neuronal Signaling Stem Cell/Wnt
  3. γ-secretase Notch
  4. Avagacestat

Avagacestat  (Synonyms: BMS-708163)

目錄號: HY-50845 純度: 99.89%
COA 產品使用指南

Avagacestat (BMS-708163) 是有效的 γ-secretase 抑制劑，抑制 Aβ42 和 Aβ40 的產生，IC50 值分別為 0.27 nM 和 0.30 nM；BMS-708163 同時抑制 Notch 胞內結構域 (NICD) 和 CYP2C19，IC50 值分別為 0.84 nM 和 20 μM。Avagacestat 可用于阿爾茲海默癥的研究。

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Avagacestat Chemical Structure

Avagacestat Chemical Structure

CAS No. : 1146699-66-2

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1353
In-stock
1 mg ￥579
In-stock
5 mg ￥1181
In-stock
10 mg ￥2232
In-stock
50 mg 現(xiàn)貨 詢價
100 mg   詢價  
200 mg   詢價  

* Please select Quantity before adding items.

  • 生物活性

  • 實驗參考方法

  • 純度 & 產品資料

  • 參考文獻

生物活性

Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (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. Avagacestat can be used for Alzheimer disease research.

IC50 & Target

IC50: 0.27 nM (γ-secretase, Aβ42), 0.30 nM (γ-secretase, Aβ40), 20 μM (CYP2C19)[1], 0.84 nM (NICD)[2]
體外研究
(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[1]. Avagacestat (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. 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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內研究
(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[1]. 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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

520.89

Formula

C20H17ClF4N4O4S
CAS 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : ≥ 100 mg/mL (191.98 mM; 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質量 1 mg 5 mg 10 mg
1 mM 1.9198 mL 9.5990 mL 19.1979 mL
5 mM 0.3840 mL 1.9198 mL 3.8396 mL
查看完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內使用， -20°C儲存時，請在1年內使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    90% Corn Oil

    Solubility: ≥ 3 mg/mL (5.76 mM); 澄清溶液

    此方案可獲得 ≥ 3 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。

    以 1 mL 工作液為例，取 100 μL 30.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網站選購。 ，Tween 80，均可在 MCE 網站選購。
計算結果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術支持聯(lián)系。
動物實驗體內工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產品資料

純度: 99.89%

參考文獻
Cell Assay
[3]

The cell viability is assessed using a tetrazolium salt (WST-8)-based colorimetric assay from the Cell Counting Kit 8 (CCK-8). The cells are seeded into 96-well plates at an initial density of 5×103 cells/well and cultured for 24?h, after which the cells are cultured with DMSO, increased concentrations of gefitinib or Avagacestat (BMS-708163) , BIBW2992, or the combination of Avagacestat (BMS-708163) and BIBW2992 for an additional 48?h. The A450 is measured in a microplate reader after 10?μL of CCK-8 solution is added and incubated for 1?h. The percentage of growth is shown relative to untreated controls.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Four- to six-week-old female Balb/c athymic (nu?+?/nu?+) mice are anesthetized with ether. The mice are acclimatized for one week before being injected with 1.5×106 PC9/AB2 cells that have been resuspended in 200?μL of matrigel. When established tumors of approximately 150-300 mm3 in diameter are detected, the mice are randomly divided into groups and fed orally by gavage with either vehicle (1% methylcellulose, 0.2% Tween 80 in sterilized water), gefitinib (3?mg/kg diluted in vehicle), Avagacestat (BMS-708163) (10?mg/kg diluted in vehicle), or a combination of gefitinib (3?mg/kg) and Avagacestat (BMS-708163) (10?mg/kg) for 5 days/week. Each treatment group consists of eight mice. The tumor volume are measured and calculated every five days using the following formula: π/6×(larger diameter)×(smaller diameter)2. After 30 days, mice are killed by cervical dislocation.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻

完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內使用， -20°C儲存時，請在1年內使用。

可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9198 mL 9.5990 mL 19.1979 mL 47.9948 mL
5 mM 0.3840 mL 1.9198 mL 3.8396 mL 9.5990 mL
10 mM 0.1920 mL 0.9599 mL 1.9198 mL 4.7995 mL
15 mM 0.1280 mL 0.6399 mL 1.2799 mL 3.1997 mL
20 mM 0.0960 mL 0.4799 mL 0.9599 mL 2.3997 mL
25 mM 0.0768 mL 0.3840 mL 0.7679 mL 1.9198 mL
30 mM 0.0640 mL 0.3200 mL 0.6399 mL 1.5998 mL
40 mM 0.0480 mL 0.2400 mL 0.4799 mL 1.1999 mL
50 mM 0.0384 mL 0.1920 mL 0.3840 mL 0.9599 mL
60 mM 0.0320 mL 0.1600 mL 0.3200 mL 0.7999 mL
80 mM 0.0240 mL 0.1200 mL 0.2400 mL 0.5999 mL
100 mM 0.0192 mL 0.0960 mL 0.1920 mL 0.4799 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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