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  2. Apoptosis
  3. Bcl-2 Family
  4. AZD-5991

AZD-5991 是一種有效的選擇性 Mcl-1 抑制劑，F(xiàn)RET 實驗檢測的 IC50 為 0.7 nM， SPR 實驗檢測的 Kd 為 0.17 nM。

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AZD-5991 Chemical Structure

AZD-5991 Chemical Structure

CAS No. : 2143061-81-6

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥4437
In-stock
1 mg ￥1500
In-stock
5 mg ￥3000
In-stock
10 mg ￥4800
In-stock
50 mg   詢價  
100 mg   詢價  

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Other Forms of AZD-5991:

查看 Bcl-2 Family 亞型特異性產(chǎn)品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

AZD-5991 is a potent and selective Mcl-1 inhibitor with an IC50 of 0.7 nM in FRET assay and a Kd of 0.17 nM in surface plasmon resonance (SPR) assay[1].

IC50 & Target[1]

Mcl-1

0.7 nM (IC50)

Mcl-1

0.17 nM (Kd)

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
K562 IC50
29.6 μM
Compound: 5; AZD5991
Antiproliferative activity against human K562 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
[PMID: 34342996]
MV4-11 IC50
0.024 μM
Compound: 5; AZD5991
Antiproliferative activity against human MV4-11 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human MV4-11 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
[PMID: 34342996]
NCI-H23 IC50
0.19 μM
Compound: 5; AZD5991
Antiproliferative activity against human NCI-H23 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H23 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
[PMID: 34342996]
NCI-H929 IC50
0.036 μM
Compound: 5; AZD5991
Antiproliferative activity against human NCI-H929 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H929 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
[PMID: 34342996]
SK-BR-3 IC50
30 μM
Compound: 5; AZD5991
Antiproliferative activity against human SK-BR-3 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human SK-BR-3 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
[PMID: 34342996]
體外研究
(In Vitro)

The selectivity of AZD-5991 is evaluated against pro-survival Bcl-2 family members using FRET assays. AZD-5991 is selective for Mcl-1 (IC50 0.72?nM, Ki=200?pM) vs. Bcl-2 (IC50=20?μM, Ki=6.8?μM), Bcl-xL (IC50=36?μM, Ki=18?μM), Bcl-w (IC50=49?μM, Ki=25?μM), and Bfl-1 (IC50=24?μM, Ki=12?μM). MOLP-8, MV4-11, and NCI-H23 cells are treated with AZD5991 (EC50=0.033, 0.024, 0.19?μM, respectively).AZD5991 binds directly to Mcl-1 and induces rapid apoptosis in cancer cells, most notably myeloma and acute myeloid leukemia, by activating the Bak-dependent mitochondrial apoptotic pathway. AZD5991 reduces the levels of Mcl-1 protein in AZD5991-sensitive but not in AZD5991-resistant MM cell lines further supporting the notion that activation of caspases by AZD5991 reduces Mcl-1 protein levels in AZD5991-sensitive cell lines[1].

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

A single intravenous (i.v.) dose of AZD5991 leads to a dose-dependent antitumor effect ranging from tumor growth inhibition (TGI) to tumor regression (TR). Ten days after treatment, AZD5991 shows 52% and 93% TGI (p<0.0001) at 10 and 30?mg/kg, respectively. At the same time point, AZD5991 at 60?mg/kg leads to 99% TR with no detectable tumors in 6 out of 7 mice, while complete TR is seen in 7 out of 7 mice in the 100?mg/kg dose group. AZD5991 also shows a dose-dependent duration of response with tumors in the 100?mg/kg group growing back later than those in the 60?mg/kg group. The magnitude of in vivo tumor efficacy is correlated with activation of caspase-3 in the tumor and concentration of AZD5991 in plasma. Treatment with AZD5991 was well tolerated at all dose levels with no significant body weight loss. A single dose of AZD5991 36 days after the first dose causes tumor regression in 4 out of 4 mice. In mice dosed with AZD5991 at 100?mg/kg on day 0 and day 1, tumors grow back later than those dosed with a single dose of AZD5991 at the same dose level[1].

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

672.26

Formula

C35H34ClN5O3S2
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 1 year
-20°C 6 months
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 250 mg/mL (371.88 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.4875 mL 7.4376 mL 14.8752 mL
5 mM 0.2975 mL 1.4875 mL 2.9750 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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(jié)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(nèi)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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.09 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.09 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
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(nèi)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(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計算結(jié)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(chǎn)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(shù)支持聯(lián)系。
動物實驗體內(nèi)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(chǎn)品資料

純度: 99.79%

參考文獻
Animal Administration
[1]

Mice and Rats[1]
In mice, drugs (e.g., AZD5991; 10-100?mg/kg) are dosed intravenously in a volume of 5?mL/kg except for Venetoclax that is dosed orally in a volume of 10?mL/kg. One million MV4-11, five million MOLP-8, ten million NCI-H929 or five million OCI-AML3 cells are injected subcutaneously in the right flank of mice in a volume of 0.1?mL. In rats, AZD5991 (10-100?mg/kg) is dosed intravenously in a volume of 10?mL/kg. Ten million MV4-11 cells are injected subcutaneously in the right flank of rats in a volume of 0.1?mL. Tumor volumes (measured by caliper), animal body weight, and tumor condition are recorded twice weekly for the duration of the study. The tumor volume is calculated[1].

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(chǎn)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(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(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 1.4875 mL 7.4376 mL 14.8752 mL 37.1880 mL
5 mM 0.2975 mL 1.4875 mL 2.9750 mL 7.4376 mL
10 mM 0.1488 mL 0.7438 mL 1.4875 mL 3.7188 mL
15 mM 0.0992 mL 0.4958 mL 0.9917 mL 2.4792 mL
20 mM 0.0744 mL 0.3719 mL 0.7438 mL 1.8594 mL
25 mM 0.0595 mL 0.2975 mL 0.5950 mL 1.4875 mL
30 mM 0.0496 mL 0.2479 mL 0.4958 mL 1.2396 mL
40 mM 0.0372 mL 0.1859 mL 0.3719 mL 0.9297 mL
50 mM 0.0298 mL 0.1488 mL 0.2975 mL 0.7438 mL
60 mM 0.0248 mL 0.1240 mL 0.2479 mL 0.6198 mL
80 mM 0.0186 mL 0.0930 mL 0.1859 mL 0.4648 mL
100 mM 0.0149 mL 0.0744 mL 0.1488 mL 0.3719 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：
AZD-5991
目錄號：
HY-101533
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