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  2. Apoptosis
  3. Bcl-2 Family
  4. VU0661013

VU661013 是一種有效的選擇性 MCL-1 抑制劑。

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VU0661013 Chemical Structure

VU0661013 Chemical Structure

CAS No. : 2131184-57-9

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥5194
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1 mg ￥1338
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5 mg ￥3313
In-stock
10 mg ￥4700
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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

VU661013 is a potent and selective MCL-1 inhibitor.

IC50 & Target

Mcl-1

 

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
AMO1 GI50
140 nM
Compound: 42; VU0661013
Antiproliferative activity against Mcl1-sensitive human AMO1 cells assessed as cell growth inhibition measured after 72 hrs by Celltiter-glo luminescence assay
Antiproliferative activity against Mcl1-sensitive human AMO1 cells assessed as cell growth inhibition measured after 72 hrs by Celltiter-glo luminescence assay
[PMID: 30929420]
B-ALL IC50
1600 nM
Compound: 42; VU0661013
Antiproliferative activity against BCR-ABL positive human B-ALL cells expressing human BFL1 assessed as reduction in cell viability after 24 hrs by Annexin-V-APC/propidium iodide staining-based flow cytometric analysis
Antiproliferative activity against BCR-ABL positive human B-ALL cells expressing human BFL1 assessed as reduction in cell viability after 24 hrs by Annexin-V-APC/propidium iodide staining-based flow cytometric analysis
[PMID: 30929420]
B-ALL IC50
2208 nM
Compound: 42; VU0661013
Antiproliferative activity against BCR-ABL positive human B-ALL cells expressing human Bcl2 assessed as reduction in cell viability after 24 hrs by Annexin-V-APC/propidium iodide staining-based flow cytometric analysis
Antiproliferative activity against BCR-ABL positive human B-ALL cells expressing human Bcl2 assessed as reduction in cell viability after 24 hrs by Annexin-V-APC/propidium iodide staining-based flow cytometric analysis
[PMID: 30929420]
B-ALL IC50
2856 nM
Compound: 42; VU0661013
Antiproliferative activity against BCR-ABL positive human B-ALL cells expressing human BFL-w assessed as reduction in cell viability after 24 hrs by Annexin-V-APC/propidium iodide staining-based flow cytometric analysis
Antiproliferative activity against BCR-ABL positive human B-ALL cells expressing human BFL-w assessed as reduction in cell viability after 24 hrs by Annexin-V-APC/propidium iodide staining-based flow cytometric analysis
[PMID: 30929420]
B-ALL IC50
3895 nM
Compound: 42; VU0661013
Antiproliferative activity against BCR-ABL positive human B-ALL cells expressing human Bcl-xl assessed as reduction in cell viability after 24 hrs by Annexin-V-APC/propidium iodide staining-based flow cytometric analysis
Antiproliferative activity against BCR-ABL positive human B-ALL cells expressing human Bcl-xl assessed as reduction in cell viability after 24 hrs by Annexin-V-APC/propidium iodide staining-based flow cytometric analysis
[PMID: 30929420]
B-ALL IC50
4186 nM
Compound: 42; VU0661013
Antiproliferative activity against BCR-ABL-positive double bax/bak knockout human B-ALL cells assessed as reduction in cell viability after 24 hrs by Annexin-V-APC/propidium iodide staining-based flow cytometric analysis
Antiproliferative activity against BCR-ABL-positive double bax/bak knockout human B-ALL cells assessed as reduction in cell viability after 24 hrs by Annexin-V-APC/propidium iodide staining-based flow cytometric analysis
[PMID: 30929420]
B-ALL IC50
446 nM
Compound: 42; VU0661013
Antiproliferative activity against BCR-ABL positive human B-ALL cells expressing human MCl1 assessed as reduction in cell viability after 24 hrs by Annexin-V-APC/propidium iodide staining-based flow cytometric analysis
Antiproliferative activity against BCR-ABL positive human B-ALL cells expressing human MCl1 assessed as reduction in cell viability after 24 hrs by Annexin-V-APC/propidium iodide staining-based flow cytometric analysis
[PMID: 30929420]
BT-20 GI50
2.1 μM
Compound: 42; VU0661013
Antiproliferative activity against human BT20 cells assessed as cell growth inhibition measured after 72 hrs by Celltiter-glo luminescence assay
Antiproliferative activity against human BT20 cells assessed as cell growth inhibition measured after 72 hrs by Celltiter-glo luminescence assay
[PMID: 30929420]
HCC1187 GI50
1.3 μM
Compound: 42; VU0661013
Antiproliferative activity against human HCC1187 cells assessed as cell growth inhibition measured after 72 hrs by Celltiter-glo luminescence assay
Antiproliferative activity against human HCC1187 cells assessed as cell growth inhibition measured after 72 hrs by Celltiter-glo luminescence assay
[PMID: 30929420]
K562 GI50
9.2 μM
Compound: P-42
Antiproliferative activity against Mcl1-insensitive human K562 cells assessed as cell growth inhibition after 72 hrs by Celltiter-glo luminescence assay
Antiproliferative activity against Mcl1-insensitive human K562 cells assessed as cell growth inhibition after 72 hrs by Celltiter-glo luminescence assay
[PMID: 30929420]
K562 GI50
9.2 μM
Compound: M-42
Antiproliferative activity against Mcl1-insensitive human K562 cells assessed as cell growth inhibition after 72 hrs by Celltiter-glo luminescence assay
Antiproliferative activity against Mcl1-insensitive human K562 cells assessed as cell growth inhibition after 72 hrs by Celltiter-glo luminescence assay
[PMID: 30929420]
K562 GI50
9.3 μM
Compound: 42; VU0661013
Antiproliferative activity against Mcl1-insensitive human K562 cells assessed as cell growth inhibition after 72 hrs by Celltiter-glo luminescence assay
Antiproliferative activity against Mcl1-insensitive human K562 cells assessed as cell growth inhibition after 72 hrs by Celltiter-glo luminescence assay
[PMID: 30929420]
MV4-11 GI50
181 nM
Compound: VU661013
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 48 hrs by CellTiter-Glo reagent based assay
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 48 hrs by CellTiter-Glo reagent based assay
[PMID: 33253879]
MV4-11 GI50
70 nM
Compound: 42; VU0661013
Antiproliferative activity against Mcl1-sensitive human MV4-11 cells assessed as cell growth inhibition measured after 72 hrs by Celltiter-glo luminescence assay
Antiproliferative activity against Mcl1-sensitive human MV4-11 cells assessed as cell growth inhibition measured after 72 hrs by Celltiter-glo luminescence assay
[PMID: 30929420]
NCI-H929 EC50
0.11 μM
Compound: M-42
Induction of apoptosis in Mcl-1 sensitive human NCI-H929 cells assessed as activation of caspase3/7 for 3 hrs by Caspase-Glo luminescence analysis
Induction of apoptosis in Mcl-1 sensitive human NCI-H929 cells assessed as activation of caspase3/7 for 3 hrs by Caspase-Glo luminescence analysis
[PMID: 30929420]
NCI-H929 GI50
0.12 μM
Compound: P-42
Antiproliferative activity against Mcl1-sensitive human NCI-H929 cells assessed as cell growth inhibition after 72 hrs by Celltiter-glo luminescence assay
Antiproliferative activity against Mcl1-sensitive human NCI-H929 cells assessed as cell growth inhibition after 72 hrs by Celltiter-glo luminescence assay
[PMID: 30929420]
NCI-H929 GI50
0.12 μM
Compound: M-42
Antiproliferative activity against Mcl1-sensitive human NCI-H929 cells assessed as cell growth inhibition after 72 hrs by Celltiter-glo luminescence assay
Antiproliferative activity against Mcl1-sensitive human NCI-H929 cells assessed as cell growth inhibition after 72 hrs by Celltiter-glo luminescence assay
[PMID: 30929420]
NCI-H929 EC50
0.13 μM
Compound: P-42
Induction of apoptosis in Mcl-1 sensitive human NCI-H929 cells assessed as activation of caspase3/7 for 3 hrs by Caspase-Glo luminescence analysis
Induction of apoptosis in Mcl-1 sensitive human NCI-H929 cells assessed as activation of caspase3/7 for 3 hrs by Caspase-Glo luminescence analysis
[PMID: 30929420]
NCI-H929 EC50
0.16 μM
Compound: 42; VU0661013
Induction of apoptosis in Mcl-1 sensitive human NCI-H929 cells assessed as activation of caspase3/7 for 3 hrs by Caspase-Glo luminescence analysis
Induction of apoptosis in Mcl-1 sensitive human NCI-H929 cells assessed as activation of caspase3/7 for 3 hrs by Caspase-Glo luminescence analysis
[PMID: 30929420]
NCI-H929 GI50
0.19 μM
Compound: 42; VU0661013
Antiproliferative activity against Mcl1-sensitive human NCI-H929 cells assessed as cell growth inhibition after 72 hrs by Celltiter-glo luminescence assay
Antiproliferative activity against Mcl1-sensitive human NCI-H929 cells assessed as cell growth inhibition after 72 hrs by Celltiter-glo luminescence assay
[PMID: 30929420]
NCI-H929 EC50
100 nM
Compound: 42; VU0661013
Induction of apoptosis in Mcl1-sensitive human NCI-H929 cells measured after 3 hrs by Caspase-glo luminescence analysis
Induction of apoptosis in Mcl1-sensitive human NCI-H929 cells measured after 3 hrs by Caspase-glo luminescence analysis
[PMID: 30929420]
體外研究
(In Vitro)

VU661013 exhibits a Ki of 97±30 pM to human MCL-1 in a TR-FRET assay by displacing a fluorescently labeled peptide derived from the pro-apoptotic protein BAK. However, VU661013 does not significantly inhibit BCL-xL (Ki>40 μM) or BCL-2 (Ki=0.73 μM)[1].

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

VU661013, a novel, potent, selective MCL-1 inhibitor that de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML, and is active in Venetoclax-resistant cells and patient derived xenografts. After establishing disseminated leukemia, NSGS mice are dosed intraperitoneally with 10, 25 or 75 mg/kg of VU661013 daily for 21 days. Weekly chimerism analyses are conducted and the percentage of MV-4-11 cells are quantified in murine peripheral blood using anti-human CD45 (hCD45) and anti-hCD33 monoclonal antibodies. Twenty-eight days post-transplant, vehicle-treated mice have developed large leukemia burdens and thus, mice are sacrificed, and their organs are harvested for analysis. Vehicle mice treated died of xenografted AML, but have no evidence of VU661013-related toxicity in non target organs. VU661013 treatment of disseminated human AML results in a dose-dependent decrease in tumor burden, nearly eliminating the hCD45+ MV-4-11 cells at the 75 mg/kg dose in the blood (mean, 13.0±2.2% in vehicle vs 7.4±7.2% in 25mg/kg vs 0.17±0.12% in 75 mg/kg treated mice), bone marrow (mean, 40.7±13.9% in vehicle vs 33.46±4.0 % in 25 mg/kg vs 0.384±0.345 in 75 mg/kg treated mice), and spleen (mean, 46.22±13.3% in vehicle vs 13.31±10.0% in 25 mg/kg vs 1.588±1.51% in 75 mg/kg treated mice). Treatment with VU661013 reduces disease-associated splenomegaly (mean, vehicle vs. 75mg/kg, 0.17±0.02 vs 0.09±0.01g), and amendeding spleen to body weight ratio (vehicle vs 75mg/kg, 0.99 vs 0.50). In a second MV-4-11 xenograft study, mice are followed until death, and survival is evaluated by Kaplan-Meier analysis. In this study, NSGS mice are treated daily (starting 7 days after transplant) with vehicle only, 15 mg/kg or 75 mg/kg of VU661013. Analysis reveals an increase in survival in mice treated with the 75mg/kg dose (vehicle treated mice=31 days, vs 15 mg/kg=32 days, vs 75 mg/kg treated mice=43 Days)[1].

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

712.66

Formula

C39H39Cl2N5O4
CAS 號
性狀

固體

顏色

Light yellow to yellow

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : ≥ 125 mg/mL (175.40 mM; 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)

* "≥" 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 1.4032 mL 7.0160 mL 14.0319 mL
5 mM 0.2806 mL 1.4032 mL 2.8064 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，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (2.92 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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (2.92 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.08 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
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(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)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(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(chǎn)品資料
參考文獻
Cell Assay
[1]

To generate cells that are resistant to BCL-2 or MCL-1 inhibition, MV-4-11 cells are treated over the course of 3 months with gradually increasing concentrations of VEN (5 nM to 2.5 μM) or VU661013 (100 nM to 5 μM). Cells are declared to be VEN or VU661013-resistant when they are able to maintain 100% viability in the presence of these high concentrations (5 μM of VU661013 and 2.5 μM of VEN) of inhibitors[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Upon establishing microchimerism, mice are treated with either Venetoclax by daily gavage, VU661013 (10, 25 or 75 mg/kg) by daily i.p injection, or vehicle. VU661013 is dissolved in DMSO and diluted in ethanol, Polyethylene Glycol (PEG), and saline. Venetoclax is dissolved in PEG and ethanol, and diluted with Phosal 50 PG. Peripheral blood is assessed weekly for human chimerism. Spleen/body ratio is calculated as organ weight (gram) per gram of body weight[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，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4032 mL 7.0160 mL 14.0319 mL 35.0798 mL
5 mM 0.2806 mL 1.4032 mL 2.8064 mL 7.0160 mL
10 mM 0.1403 mL 0.7016 mL 1.4032 mL 3.5080 mL
15 mM 0.0935 mL 0.4677 mL 0.9355 mL 2.3387 mL
20 mM 0.0702 mL 0.3508 mL 0.7016 mL 1.7540 mL
25 mM 0.0561 mL 0.2806 mL 0.5613 mL 1.4032 mL
30 mM 0.0468 mL 0.2339 mL 0.4677 mL 1.1693 mL
40 mM 0.0351 mL 0.1754 mL 0.3508 mL 0.8770 mL
50 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7016 mL
60 mM 0.0234 mL 0.1169 mL 0.2339 mL 0.5847 mL
80 mM 0.0175 mL 0.0877 mL 0.1754 mL 0.4385 mL
100 mM 0.0140 mL 0.0702 mL 0.1403 mL 0.3508 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：
VU0661013
目錄號：
HY-112859
需求量：