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  3. OTSSP167 hydrochloride

OTSSP167 hydrochloride  (Synonyms: OTS167 hydrochloride)

目录号: HY-15512A 纯度: 99.84%
COA 产品使用指南

OTSSP167 (OTS167) hydrochloride 是一种高效的,ATP 竞争性的 MELK 抑制剂,IC50 值为 0.41 nM。

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OTSSP167 hydrochloride Chemical Structure

OTSSP167 hydrochloride Chemical Structure

CAS No. : 1431698-10-0

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10 mM * 1 mL in DMSO ¥1150
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1 mg ¥454
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5 mg ¥1000
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10 mg ¥1500
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25 mg ¥2475
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50 mg ¥4500
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100 mg ¥6412
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Other Forms of OTSSP167 hydrochloride:

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Top Publications Citing Use of Products

    OTSSP167 hydrochloride purchased from MCE. Usage Cited in: Blood Cancer J. 2019 Nov 18;9(12):87.  [Abstract]

    Expression of MELK and Aurora B kinase (AurB) is determined in samples from vehicle and OTSSP167-treated mice. β-actin is used as loading control.

    OTSSP167 hydrochloride purchased from MCE. Usage Cited in: Clin Cancer Res. 2018 Nov 15;24(22):5645-5657.  [Abstract]

    Western blot showing protein levels of MELK, PPARγ and phospho-PPARγS112 in JHH-DIPG-01, HSJD-DIPG-12, SF7761 and HSJD-DIPG-07 cells after 48 hours treatment with either 20 nM or 50 nM OTSSP167.

    OTSSP167 hydrochloride purchased from MCE. Usage Cited in: EMBO Mol Med. 2018 Mar;10(3). pii: e8274.  [Abstract]

    Validation of effects of OTS167 on phosphorylation of p90RSK and its targets. C4-2b cells are treated with vehicle or 30 nM OTS167 for the indicated times, and levels of total and phosphorylated proteins are determined by Western blot analysis. β-Actin is used as a loading control.

    OTSSP167 hydrochloride purchased from MCE. Usage Cited in: Gynecol Oncol. 2017 Apr;145(1):159-166.  [Abstract]

    Western blotting demonstrates that 100 nM OTSSP167 for 48 h produces marked PARP-1 cleavage in HGSOC cell lines whereas no or weak PARP-1 cleavage is observed in normal ovarian surface epithelial cells (HOSE6-3) and in the fallopian tubal cells (FT33-tag, FT190, FT237).

    OTSSP167 hydrochloride purchased from MCE. Usage Cited in: Sci Rep. 2017 Feb 14;7:42502.  [Abstract]

    In vitro kinase assays are performed using MPK38 immunoprecipitates, which are obtained from cell lysates of wild-type and clonal CRISPR/Cas9 ZPR9 (T252A) KI isolates, treated with (+) or without (−) OTSSP167 (1 μM, 2 h), a MPK38-specific inhibitor, in the presence of ZPR9 immunoprecipitates as the substrate. Recombinant MPK38 proteins (lower panels), which were expressed in bacterial cells, treated with (+) or without (−) OTSSP167 are also used instead of the MPK38 immunoprecipitates (upper pan

    OTSSP167 hydrochloride purchased from MCE. Usage Cited in: PLoS One. 2017 Feb 24;12(2):e0172832.  [Abstract]

    OTS167 reduces proliferation and regulates MELK transcript but not protein levels in TNBC cells. The MELK 52 kDa variant is highly expressed in the TNBC cell lines but not in luminal A MCF-7.

    OTSSP167 hydrochloride purchased from MCE. Usage Cited in: Oncotarget. 2017 Dec 20;9(2):2591-2602.  [Abstract]

    Effects of OTSSP167 on PARP and Caspase-3 cleavages in NB cells are shown by immunoblotting assay.

    OTSSP167 hydrochloride purchased from MCE. Usage Cited in: Patent. US20160291017A1.

    Mitotic MDA-MB-468 cells are treated for 30 min with vehicle or 200 nM OTSSP167, a MELK inhibitor. Lysates are used for immunoblotting.

    OTSSP167 hydrochloride purchased from MCE. Usage Cited in: Mol Cancer. 2014 May 4;13:100.  [Abstract]

    MELK specific inhibitor OTSSP167 suppresses cell migration and invasion. A, Immunoblotting representing MELK expression in SGC7901 cell following OTSSP167 treatment for indicated period. In the upper panel, SGC7901 cell are treated with different concentration (0, 0.1, 1 μM) of OTSSP167 for 1 h and 2 h. In the lower panel, SGC7901/vector and SGC7901/MELK cell are treated with 1 μM OTSSP167 for 2 h. C, SGC7901/vector and SGC7901/MELK cells are treated with 1 μM OTSSP167 for indicated period and
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    OTSSP167 (OTS167) hydrochloride is a highly potent and ATP-competitive MELK inhibitor with IC50 value of 0.41 nM.

    IC50 & Target

    IC50: 0.41 nM (MELK)

    体外研究
    (In Vitro)

    OTSSP167 inhibits the growth of A549 (lung), T47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC50 values of 6.7, 4.3, 2.3, 6.0 and 97 nM, respectively[1].
    OTSSP167 can abrogate the mitotic checkpoint, disrupt MCC and MCC-APC/C interaction in MCF7 cells. OTSSP167 causes GFP-MELK localization to cell cortex in prometaphase cells[2].
    OTSSP167 is a MELK selective inhibitor, exhibits a strong in vitro activity, conferring an IC50 of 0.41 nM[3].

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

    体内研究
    (In Vivo)

    OTSSP167 (20 mg/kg, i.v.) results in tumor growth inhibition (TGI) of 73% in xenograft mouse model; OTSSP167 (1, 5, and 10 mg/kg, p.o.) reveals TGI of 51, 91, and 108%, respectively. OTSSP167 (20 mg/kg, p.o.) shows no tumor growth suppressive effect on PC-14 xenografts[1].

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

    分子量

    523.88

    Formula

    C25H29Cl3N4O2

    CAS 号
    性状

    固体

    颜色

    Light yellow to gray

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 33.33 mg/mL (63.62 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : 7.14 mg/mL (13.63 mM; 超声助溶)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9088 mL 9.5442 mL 19.0883 mL
    5 mM 0.3818 mL 1.9088 mL 3.8177 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 3 mg/mL (5.73 mM); 澄清溶液

      此方案可获得 ≥ 3 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 3 mg/mL (5.73 mM); 澄清溶液

      此方案可获得 ≥ 3 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂: PBS

      Solubility: 1 mg/mL (1.91 mM); 澄清溶液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.84%

    参考文献
    Kinase Assay
    [1]

    For in vitro kinase assay, MELK recombinant protein (0.4 μg) is mixed with 5 μg of each substrate in 20 μL of kinase buffer containing 30 mM Tris-HCl (pH), 10 mM DTT, 40 mM NaF, 10 mM MgCl2, 0.1 mM EGTA with 50 μM cold-ATP and 10 Ci of [γ-32P]ATP for 30 min at 30°C. The reaction Is terminated by addition of SDS sample buffer and boiled for 5 min prior to SDS-PAGE. The gel is dried and autoradiographed with intensifying screens at room temperature. OTSSP167 (final concentration of 10 nM) is dissolved in DMSO and added to kinase buffer before the incubation.

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

    Cell Assay
    [1]

    In vitro cell viability is measured by the colorimetric assay using Cell Counting Kit-8. Cells are plated in 100 μL in 96-well plates at a density that generates continual linear growth (A549, 1×103 cells; T47D, 3×103 cells; DU4475, 4×103 cells; 22Rv1, 6×103 cells; and HT1197, 2×103 cells, in 100 μL per well). The cells are allowed to adhere overnight before exposure to OTSSP167 for 72 hours at 37°C. Plates are read using a spectrophotometer at a wavelength of 450 nm. All assays are carried out in triplicate.

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

    Animal Administration
    [1]

    MDA-MB-231 cells are injected into the mammary fat pads of NOD.CB17-Prkdcscid/J mice. A549, MIAPaCa-2 and PC-14 cells (1×105 cells) are injected subcutaneously in the left flank of female BALB/cSLC-nu/nu mice. DU145 cells are injected subcutaneously in the left flank of male BALB/cSLC-nu/nu mice. When MDA-MB-231, A549, DU145, MIAPaCa-2, and PC-14 xenografts has reached an average volume of 100, 210, 110, 250, and 250 mm3, respectively, animals are randomized into groups of 6 mice (except for PC-14, for which groups of 3 mice are used). For oral administration, OTSSP167 and other compounds are prepared in a vehicle of 0.5% methylcellulose and given by oral garbage at the indicated dose and schedule. For intravenous administration, compounds are formulated in 5% glucose and injected into the tail vein. An administration volume of 10 mL per kg of body weight is used for both administration routes. Tumor volumes are determined every other day using a caliper.

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

    参考文献

    OTSSP167 hydrochloride 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.9088 mL 9.5442 mL 19.0883 mL 47.7209 mL
    5 mM 0.3818 mL 1.9088 mL 3.8177 mL 9.5442 mL
    10 mM 0.1909 mL 0.9544 mL 1.9088 mL 4.7721 mL
    DMSO 15 mM 0.1273 mL 0.6363 mL 1.2726 mL 3.1814 mL
    20 mM 0.0954 mL 0.4772 mL 0.9544 mL 2.3860 mL
    25 mM 0.0764 mL 0.3818 mL 0.7635 mL 1.9088 mL
    30 mM 0.0636 mL 0.3181 mL 0.6363 mL 1.5907 mL
    40 mM 0.0477 mL 0.2386 mL 0.4772 mL 1.1930 mL
    50 mM 0.0382 mL 0.1909 mL 0.3818 mL 0.9544 mL
    60 mM 0.0318 mL 0.1591 mL 0.3181 mL 0.7953 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    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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    产品名称:
    OTSSP167 hydrochloride
    目录号:
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