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  2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. BS-181

BS-181 是一種有效的 CDK7 選擇性抑制劑 (IC50=21 nM)，與 Seliciclib (HY-30237) 相比。BS-181 抑制CDK2、CDK5 和 CDK9 的 IC50 值分別為 880 nM、3000 nM 和 4200 nM (不能阻斷 CDK1、4 和 6)。BS-181 抑制一組癌細胞生長 (IC50=11.5 μM-37.3 μM)，誘導細胞凋亡 (apoptosis)。BS-181 具有癌癥研究相關研究的潛力。

該游離形式化合物不穩(wěn)定，推薦具有相同生物學活性的穩(wěn)定鹽形式 BS-181 hydrochloride。

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BS-181 Chemical Structure

BS-181 Chemical Structure

CAS No. : 1092443-52-1

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規(guī)格 價格 是否有貨
5 mg ￥800
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BS-181 的其他形式現(xiàn)貨產(chǎn)品:

Customer Review

Other Forms of BS-181:

    BS-181 purchased from MCE. Usage Cited in: Theranostics. 2017 Apr 20;7(7):1914-1927.  [Abstract]

    Effect of TPL on the levels of pAR S515 and related proteins in PCa cells. LNCaP and C4-2/AR-V7 cells are pretreated with TPL or BS-181 for 1 h, and then incubated with R1881 for 4 h.

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    BS-181 is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880, 3000 and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 has the potential for the research of cancer therapy[1][2].

    IC50 & Target[1]

    CDK7/CycH/MAT1

    0.021 μM (IC50)

    CDK2/Cyc E

    0.88 μM (IC50)

    CDK1/cycB

    8.1 μM (IC50)

    CDK4/Cyc D1

    33 μM (IC50)

    CDK5/p35NCK

    3 μM (IC50)

    CDK6/cycD1

    47 μM (IC50)

    CDK9/cycT

    4.2 μM (IC50)

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    BT-549 IC50
    12.82 μM
    Compound: 1
    Growth inhibition of human BT-549 cells assessed as cell viability measured after 4 days by WST8 assay
    Growth inhibition of human BT-549 cells assessed as cell viability measured after 4 days by WST8 assay
    		[PMID: 34538051]
    MDA-MB-231 IC50
    18.47 μM
    Compound: 1
    Growth inhibition of human MDA-MB-231 cells assessed as cell viability measured after 4 days by WST8 assay
    Growth inhibition of human MDA-MB-231 cells assessed as cell viability measured after 4 days by WST8 assay
    		[PMID: 34538051]
    MDA-MB-468 IC50
    16.3 μM
    Compound: 1
    Growth inhibition of human MDA-MB-468 cells assessed as cell viability measured after 4 days by WST8 assay
    Growth inhibition of human MDA-MB-468 cells assessed as cell viability measured after 4 days by WST8 assay
    		[PMID: 34538051]
    Sf9 IC50
    1.8 μM
    Compound: BS-181
    Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP
    Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP
    		[PMID: 26851505]
    Sf9 IC50
    14 μM
    Compound: BS-181
    Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP
    Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP
    		[PMID: 26741853]
    體外研究
    (In Vitro)

    BS-181 (0-40 μM; 72 hours) inhibits cancer cells growth, it is against Breast cancer cell lines growth with IC50 values ranging from 15.1 μM to 20 μM, it is against Colorectal cancer cell lines growth with IC50 values ranging from 11.5 μM to15.3 μM and is against lung, osteosarcoma, prostate and liver cancer cell lines with IC50 values ranging from 11.5 μM to 37.3 μM, respectively[1].
    BS-181 (0-50 μM; 4 hours) shows inhibition of phosphorylation of the RNA polymerase II C-terminal domain (CTD) at serine 5 (P-Ser5). It down-regulates CDK4 and cyclin D1 expression while does not effect other CDKs and cyclins[1].
    BS-181 (0-50 μM; 24 hours) shows an increase in cells in G1, accompanied by a reduction in cell numbers in S and G2/M at low concentrations. At higher concentrations, however, cells accumulates in the sub-G1, indicative of apoptosis[1].

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

    Cell Proliferation Assay[1]

    Cell Line: Breast cancer cell line: MCF-7, MDA-MB-231, T47D, ZR-75-1, etc
    Colorectal cancer cell line: COLO-205, HCT-116, HCT-116 (p53-/-)
    Lung cancer cell line: A549, NCI-460
    Osteosarcoma cancer cell line: U2OS, SaOS2
    Prostate cancer cell line: PC3, LNCaP
    Concentration: 0-50 μM
    Incubation Time: 4 hours
    Result: Had anti-proliferative activities against a panel of cell lines, including breast, lung, prostate and colorectal cancer.

    Western Blot Analysis[1]

    Cell Line: MCF-7 cells
    Concentration: 0-40 μM
    Incubation Time: 72 hours
    Result: Inhibited phosphorylation of CDK7 substrates.

    Apoptosis Analysis[1]

    Cell Line: MCF-7 cells
    Concentration: 0-50 μM
    Incubation Time: 24 hours
    Result: Led cells to G1 arrest and apoptosis.
    體內研究
    (In Vivo)

    BS-181 (intraperitoneal injection; 5 mg/kg or 10 mg/kg twice daily; total daily doses of 10 mg/kg or 20 mg/kg; 14 days) inhibitstumor growth in a dose-dependent manner.?Tumor growth exhibits 25% and 50% reduction compared with the control group, for 10 mg/kg/day and 20 mg/kg/day, respectively[1].

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

    Animal Model: 7-week old female nu/nu-BALB/c athymic nude mice?with MCF-7 cells[1]
    Dosage: 5 mg/kg or 10 mg/kg; 10 mg/kg or 20 mg/kg
    Administration: Intraperitoneal injection; twice daily or once total daily; 14 days
    Result: Inhibited tumor growth significantly.
    分子量

    380.53

    Formula

    C22H32N6
    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 (131.40 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 2.6279 mL 13.1396 mL 26.2791 mL
    5 mM 0.5256 mL 2.6279 mL 5.2558 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, 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 3 mg/mL (7.88 mM); 澄清溶液

      此方案可獲得 ≥ 3 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 30.0 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: ≥ 3 mg/mL (7.88 mM); 澄清溶液

      此方案可獲得 ≥ 3 mg/mL（飽和度未知）的澄清溶液。

      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 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

    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, 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 2.6279 mL 13.1396 mL 26.2791 mL 65.6978 mL
    5 mM 0.5256 mL 2.6279 mL 5.2558 mL 13.1396 mL
    10 mM 0.2628 mL 1.3140 mL 2.6279 mL 6.5698 mL
    15 mM 0.1752 mL 0.8760 mL 1.7519 mL 4.3799 mL
    20 mM 0.1314 mL 0.6570 mL 1.3140 mL 3.2849 mL
    25 mM 0.1051 mL 0.5256 mL 1.0512 mL 2.6279 mL
    30 mM 0.0876 mL 0.4380 mL 0.8760 mL 2.1899 mL
    40 mM 0.0657 mL 0.3285 mL 0.6570 mL 1.6424 mL
    50 mM 0.0526 mL 0.2628 mL 0.5256 mL 1.3140 mL
    60 mM 0.0438 mL 0.2190 mL 0.4380 mL 1.0950 mL
    80 mM 0.0328 mL 0.1642 mL 0.3285 mL 0.8212 mL
    100 mM 0.0263 mL 0.1314 mL 0.2628 mL 0.6570 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：
    BS-181
    目錄號：
    HY-13266
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