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  2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. Onalespib

Onalespib (AT13387) 是一種長效的二代 Hsp90 抑制劑，Kd 值為 0.71 nM。

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Onalespib Chemical Structure

Onalespib Chemical Structure

CAS No. : 912999-49-6

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥973
In-stock
1 mg ￥490
In-stock
5 mg ￥1080
In-stock
10 mg ￥1674
In-stock
25 mg ￥2850
In-stock
50 mg ￥4200
In-stock
100 mg 現(xiàn)貨 詢價
500 mg 現(xiàn)貨 詢價
1 g   詢價  
5 g   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Onalespib:

    Onalespib purchased from MCE. Usage Cited in: Sci Rep. 2017 Mar 15;7(1):201.  [Abstract]

    For the caspase 3/7 assay, the HSP90 inhibitor-treated 5637 or SV-HUC cells are stained with Nexcelom ViaStain Caspase 3/7 reagent and Hoechst 33342. Caspase 3/7 positive cells are identified using the Celigo imaging cytometer, and the percentage of apoptotic caspase 3/7 positive cells is calculated with the Celigo software.

    查看 HSP 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

    Onalespib (AT13387) is a long-acting second-generation Hsp90 inhibitor with a Kd of 0.71 nM.

    IC50 & Target[1]

    HSP90

    0.71 nM (Kd)

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    0.05 μM
    Compound: 8; AT13387
    Antiproliferative activity against human A549 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A549 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27933959]
    A549 IC50
    0.44 μM
    Compound: AT13387
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    		[PMID: 30784881]
    BT-474 IC50
    0.032 μM
    Compound: 8; AT13387
    Antiproliferative activity against human BT-474 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human BT-474 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27933959]
    GIST430 IC50
    34 nM
    Compound: 8; AT-13387
    Cytotoxicity against imatinib-resistant human GIST430 cells assessed as decrease in cell viability after 7 days by alamar blue assay
    Cytotoxicity against imatinib-resistant human GIST430 cells assessed as decrease in cell viability after 7 days by alamar blue assay
    		[PMID: 26844689]
    GIST48 IC50
    55 nM
    Compound: 8; AT-13387
    Cytotoxicity against imatinib-resistant human GIST48 cells assessed as decrease in cell viability after 7 days by alamar blue assay
    Cytotoxicity against imatinib-resistant human GIST48 cells assessed as decrease in cell viability after 7 days by alamar blue assay
    		[PMID: 26844689]
    HCT-116 IC50
    0.07 μM
    Compound: 8; AT13387
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27933959]
    HCT-116 IC50
    0.08 μM
    Compound: AT-13387
    Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
    		[PMID: 24763261]
    HCT-116 IC50
    48 nM
    Compound: 35
    Cytotoxicity against human HCT116 cells by Alamar blue assay
    Cytotoxicity against human HCT116 cells by Alamar blue assay
    		[PMID: 20662534]
    HepG2 IC50
    0.018 μM
    Compound: 8; AT13387
    Antiproliferative activity against human HepG2 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HepG2 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27933959]
    K562 IC50
    0.038 μM
    Compound: 8; AT13387
    Antiproliferative activity against human K562 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human K562 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27933959]
    L02 IC50
    11.64 μM
    Compound: 8; AT13387
    Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27933959]
    MCF7 IC50
    0.02 μM
    Compound: 8; AT13387
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27933959]
    MCF7 IC50
    0.032 μM
    Compound: AT13387
    Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
    		[PMID: 29028527]
    MCF7 IC50
    0.28 μM
    Compound: AT-13387
    Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
    		[PMID: 24763261]
    MCF7 IC50
    0.29 μM
    Compound: AT13387
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    		[PMID: 30784881]
    MDA-MB-231 IC50
    0.038 μM
    Compound: 8; AT13387
    Antiproliferative activity against human MDA-MB-231 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27933959]
    MDA-MB-468 IC50
    0.066 μM
    Compound: 8; AT13387
    Antiproliferative activity against human MDA-MB-468 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-468 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27933959]
    MKN-28 IC50
    0.129 μM
    Compound: 8; AT13387
    Antiproliferative activity against human MKN-28 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MKN-28 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27933959]
    MV4-11 IC50
    0.011 μM
    Compound: 8; AT13387
    Antiproliferative activity against human MV4-11 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MV4-11 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27933959]
    NCI-H1299 IC50
    0.37 μM
    Compound: AT13387
    Antiproliferative activity against human NCI-H1299 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1299 cells after 72 hrs by MTT assay
    		[PMID: 30784881]
    NCI-H3122 IC50
    52 nM
    Compound: AT13387
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB assay
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB assay
    		[PMID: 29698859]
    SK-BR-3 IC50
    0.045 μM
    Compound: AT13387
    Antiproliferative activity against human SKBR3 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human SKBR3 cells incubated for 72 hrs by MTT assay
    		[PMID: 29028527]
    SK-BR-3 IC50
    0.071 μM
    Compound: 8; AT13387
    Antiproliferative activity against human SK-BR-3 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human SK-BR-3 assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27933959]
    SK-BR-3 IC50
    0.14 μM
    Compound: AT-13387
    Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay
    Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay
    		[PMID: 24763261]
    T47D IC50
    0.024 μM
    Compound: 8; AT13387
    Antiproliferative activity against human T47D assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human T47D assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27933959]
    U2OS IC50
    0.067 μM
    Compound: 8; AT13387
    Antiproliferative activity against human U2OS assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human U2OS assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27933959]
    體外研究
    (In Vitro)

    Onalespib (Compound 35) is a potent inhibitor of Hsp90, with Kd of 0.71 nM. Onalespib shows potent antiproliferative activity in HCT116 cells, with an IC50 of 31 nM. Onalespib also strongly inhibits the proliferation of a panel of human tumor cell lines, showing IC50 of < 100 nM[1]. Onalespib exhibits cytotoxic activity against many of the PPTP cell lines, with median IC50 of 41 nM[2].

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

    Onalespib (60 mg/kg, ip 3 days on and 3 days off for four cycles) shows antitumor activity in nude BALB/c mice bearing early stage HCT116 human colon carcinoma xenografts[1]. Onalespib (40 or 60 mg/kg, i.p.) induces significant differences in EFS distribution compared to controls in 17% evaluable solid tumor xenografts, but in none of the ALL xenografts[2].

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

    409.52

    Formula

    C24H31N3O3
    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 : 50 mg/mL (122.09 mM; 超聲助溶 (<60°C); 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 2.4419 mL 12.2094 mL 24.4188 mL
    5 mM 0.4884 mL 2.4419 mL 4.8838 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, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(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(dāng)?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(dāng)保存；體內(nèi)實驗的工作液，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: ≥ 2.5 mg/mL (6.10 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.10 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 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。

    以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 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： 50% PEG300    50% Saline

      Solubility: 16.67 mg/mL (40.71 mM); 懸濁液; 超聲助溶

    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
    參考文獻
    Cell Assay
    [2]

    In vitro testing is performed using DIMSCAN. Cells are incubated in the presence of Onalespib for 96 hours at concentrations from 1 nM to 10 μM[2].

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

    HCT116 cells are injected SC into the right hind flank of male nude BALB/c mice. Tumours are apparent 7 to 10 days later. Mice are arranged into matched groups of 12 according to tumour volume giving a group mean of approximately 100 mm[3] at initiation of dosing. Tumour volumes are measured every 2 days. Statistical significance between groups is assessed using nonparametric one-way ANOVA. Mice are given the lactate salt of Onalespib using a repeated cycle of dosing of once per day for three days, no dose for three days, once per day for three days etc., for four dosing cycles at 60 mg/kg/dose (as free base equivalents) dissolved in 17.5% hydroxypropyl-β-cyclodextrin via the IP route. Control mice receive dose vehicle only via the same route. Tolerability is assessed by recording body weight, clinical observations and survival[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, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1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 2.4419 mL 12.2094 mL 24.4188 mL 61.0471 mL
    5 mM 0.4884 mL 2.4419 mL 4.8838 mL 12.2094 mL
    10 mM 0.2442 mL 1.2209 mL 2.4419 mL 6.1047 mL
    15 mM 0.1628 mL 0.8140 mL 1.6279 mL 4.0698 mL
    20 mM 0.1221 mL 0.6105 mL 1.2209 mL 3.0524 mL
    25 mM 0.0977 mL 0.4884 mL 0.9768 mL 2.4419 mL
    30 mM 0.0814 mL 0.4070 mL 0.8140 mL 2.0349 mL
    40 mM 0.0610 mL 0.3052 mL 0.6105 mL 1.5262 mL
    50 mM 0.0488 mL 0.2442 mL 0.4884 mL 1.2209 mL
    60 mM 0.0407 mL 0.2035 mL 0.4070 mL 1.0175 mL
    80 mM 0.0305 mL 0.1526 mL 0.3052 mL 0.7631 mL
    100 mM 0.0244 mL 0.1221 mL 0.2442 mL 0.6105 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：
    Onalespib
    目錄號：
    HY-14463
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