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

Avagacestat (BMS-708163) 是有效的 γ-secretase 抑制劑，抑制 Aβ42 和 Aβ40 的產(chǎn)生，IC50 值分別為 0.27 nM 和 0.30 nM；BMS-708163 同時(shí)抑制 Notch 胞內(nèi)結(jié)構(gòu)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(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1340
In-stock
1 mg ￥579
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5 mg ￥1169
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10 mg ￥1868
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25 mg ￥3740
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50 mg ￥5775
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100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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]
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO ED50
1.2 nM
Compound: 43
Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA
Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA
[PMID: 23713656]
CHO ED50
71 nM
Compound: 43
Inhibition of gamma-secretase in CHO cells assessed expressing NotchdeltaE assessed as inhibition of notch cleavage after overnight incubation by luciferase reporter gene assay
Inhibition of gamma-secretase in CHO cells assessed expressing NotchdeltaE assessed as inhibition of notch cleavage after overnight incubation by luciferase reporter gene assay
[PMID: 23713656]
CHO IC50
71 nM
Compound: BMS-708163
Inhibition of gamma-secretase in CHO cells after overnight incubation by luciferase reporter gene assay
Inhibition of gamma-secretase in CHO cells after overnight incubation by luciferase reporter gene assay
[PMID: 23312944]
HEK293 ED50
1.2 nM
Compound: BMS-708163
Inhibition of gamma-secretase in HEK293 cells after overnight incubation by Western blotting analysis
Inhibition of gamma-secretase in HEK293 cells after overnight incubation by Western blotting analysis
[PMID: 23312944]
IMR-32 IC50
0.13 nM
Compound: BMS-708163
Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA
Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA
[PMID: 23312944]
IMR-32 IC50
1.5 nM
Compound: BMS-708163
Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA
Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA
[PMID: 23312944]
體外研究
(In Vitro)

Avagacestat 表現(xiàn)出較弱的 Notch 加工抑制效力，與其抑制 APP 裂解的效力相比，IC50=58±23 nM[1]。Avagacestat (10 μM) 與 Gefitinib 聯(lián)合顯著減弱 PC9/AB2 細(xì)胞的集落生長(zhǎng)，增加活性 caspase 3 和 PARP 的表達(dá)，并降低 PC9/AB2 細(xì)胞中 Ki-67 的表達(dá)。Avagacestat 在 PC9/AB2 細(xì)胞中誘導(dǎo)細(xì)胞凋亡并增強(qiáng)細(xì)胞周期停滯在 G1 期。Avagacestat 處理有效下調(diào) PC9/AB2 細(xì)胞中 Notch1、HES1、PI3K 和 Akt 的表達(dá)[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

在整個(gè)給藥間隔內(nèi)，Avagacestat 相對(duì)于對(duì)照組在 10 和 100 mg/kg 時(shí)顯著降低血漿和腦 Aβ40 水平，在口服 1 mg/kg 劑量后 8 小時(shí)內(nèi)表現(xiàn)出顯著的 Aβ40 降低，并且顯著降低單次口服劑量范圍為 3 至 100 mg/kg 后 5 小時(shí)測(cè)量的大鼠 CSF Aβ40 水平[1]。與單獨(dú)使用 Gefitinib (HY-50895) 相比，Avagacestat (10 mg/kg) 單一療法對(duì) PC9/AB2 腫瘤生長(zhǎng)具有輕微的抑制作用。BMS-708163 單一療法導(dǎo)致體內(nèi) caspase 3 表達(dá)輕微增加以及 Ki-67 表達(dá)輕微降低。在用 Avagacestat 加 Gefitinib 處理的異種移植肺癌樣本中，caspase 3 表達(dá)顯著增加，Ki-67 染色減少[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(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)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(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 100 mg/mL (191.98 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)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(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)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(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

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

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)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(guò) 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)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(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)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(chǎn)品資料

純度: 99.89%

參考文獻(xiàn)
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(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱：
Avagacestat
目錄號(hào)：
HY-50845
需求量：