2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. Samuraciclib hydrochloride hydrate

Samuraciclib hydrochloride hydrate  (Synonyms: CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate)

目录号: HY-103712C 纯度: 98.60%
COA 产品使用指南

摩尔计算器

Samuraciclib (CT7001) hydrochloride hydrate 是一种有效的，具有选择性，ATP 竞争性和口服活性的 CDK7 抑制剂，IC50 为 41 nM。Samuraciclib hydrochloride hydrate 对 CDK7 的选择性分别是 CDK1，CDK2 (IC50 为 578 nM)，CDK5 和 CDK9 的 45 倍，15 倍，230 倍和 30 倍。Samuraciclib hydrochloride hydrate 以 GI50 值为 0.2-0.3 µM 来抑制乳腺癌细胞系的生长，具有有效的抗肿瘤作用。

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Samuraciclib hydrochloride hydrate Chemical Structure

Samuraciclib hydrochloride hydrate Chemical Structure

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3038
In-stock
5 mg ￥2500
In-stock
10 mg ￥4200
In-stock
25 mg ￥8600
In-stock
50 mg   询价  
100 mg   询价  

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Other Forms of Samuraciclib hydrochloride hydrate:

Samuraciclib hydrochloride hydrate 相关抗体

Top Publications Citing Use of Products

    Samuraciclib hydrochloride hydrate purchased from MCE. Usage Cited in: J Cancer Res Clin Oncol. 2022 Nov 18.  [Abstract]

    Colony-formation assay. Samuraciclib (5, 10, 20, 50, 100 nM; 7 days) signifcantly inhibits the colony-formation ability of the two CRPC models (C4-2 and 22RV1).

    查看 CDK 亚型特异性产品:

    查看所有亚型
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride hydrate has anti-tumor effects[1][2].

    IC50 & Target[1][2]

    CDK7/CycH/MAT1

    41 nM (IC50)

    CDK2/cycE1

    578 nM (IC50)

    CDK1

    1.8 μM (IC50)

    CDK4

    49 μM (IC50)

    CDK5

    9.4 μM (IC50)

    CDK6

    34 μM (IC50)

    CDK9

    1.2 μM (IC50)

    体外研究
    (In Vitro)

    Samuraciclib (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) hydrochloride hydrate treatment promotes cell apoptosis[1].
    Samuraciclib (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) hydrochloride hydrate treatment induces cell cycle arrest[1].
    Samuraciclib (ICEC0942; 0-10 µM; 0-24 hours; HCT116 cells) hydrochloride hydrate treatment inhibits the phosphorylation of PolII CTD in a dose and time dependent manner in HCT116 colon cancer cells. Samuraciclib hydrochloride hydrate also inhibits phosphorylation of CDK1, CDK2 and retinoblastoma[1].
    Samuraciclib (ICEC0942) hydrochloride hydrate inhibits the growth of MCF7, T47D, MDA-MB-231, HS578T, MDA-MB-468, MCF10A and HMEC cells with GI50 values of 0.18 µM, 0.32 µM, 0. 33 µM, 0.21 µM, 0.22 µM, 0.67 µM and 1.25 µM, respectively[1].

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

    Samuraciclib hydrochloride hydrate 相关抗体:

    Apoptosis Analysis[1]

    Cell Line: HCT116 cells
    Concentration: 0 µM, 0.1 µM, 1 µM and 10 µM
    Incubation Time: 24 hours
    Result: Induced caspase 3/7 and demonstrated PARP cleavage.

    Cell Cycle Analysis[1]

    Cell Line: HCT116 cells
    Concentration: 0 µM, 0.1 µM, 1 µM and 10 µM
    Incubation Time: 24 hours
    Result: Showed accumulation of cells in G2/M.

    Western Blot Analysis[1]

    Cell Line: HCT116 cells
    Concentration: 0 µM, 0.1 µM, 1 µM and 10 µM
    Incubation Time: 0 hour, 4 hours, 8 hours, 16 hours or 24 hours
    Result: PolII CTD phosphorylation was inhibited in a dose and time dependent manner in HCT116 colon cancer cells.
    体内研究
    (In Vivo)

    Samuraciclib (ICEC0942; 100 mg/kg; oral gavage; daily; for 14 days; female nu/nu-BALB/c athymic nude mice) hydrochloride hydrate treatment inhibits tumor growth by 60% at day 14, and is accompanied by highly significant reductions in PolII Ser2 and Ser5 phosphorylation in PBMCs and in tumors[1].
    The combination of Samuraciclib (ICEC0942) and ICI 47699 treatment shows complete growth arrest of estrogen receptor (ER)-positive tumor xenografts[1].

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

    Animal Model: Female nu/nu-BALB/c athymic nude mice (7-week old) with MCF7 cells[1].
    Dosage: 100 mg/kg
    Administration: Oral gavage; daily; for 14 days
    Result: At day 14, tumor growth was inhibited by 60%.
    Clinical Trial
    分子量

    552.33

    Formula

    C22H33ClN6O2
    性状

    固体

    颜色

    White to light yellow

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (181.05 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)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.8105 mL 9.0526 mL 18.1051 mL
    5 mM 0.3621 mL 1.8105 mL 3.6210 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    • 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

    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

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 99.88%

    COA (270 KB) HNMR (303 KB) LCMS (293 KB)

    产品使用指南 (1538 KB)
    参考文献

    Samuraciclib hydrochloride hydrate 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8105 mL 9.0526 mL 18.1051 mL 45.2628 mL
    5 mM 0.3621 mL 1.8105 mL 3.6210 mL 9.0526 mL
    10 mM 0.1811 mL 0.9053 mL 1.8105 mL 4.5263 mL
    15 mM 0.1207 mL 0.6035 mL 1.2070 mL 3.0175 mL
    20 mM 0.0905 mL 0.4526 mL 0.9053 mL 2.2631 mL
    25 mM 0.0724 mL 0.3621 mL 0.7242 mL 1.8105 mL
    30 mM 0.0604 mL 0.3018 mL 0.6035 mL 1.5088 mL
    40 mM 0.0453 mL 0.2263 mL 0.4526 mL 1.1316 mL
    50 mM 0.0362 mL 0.1811 mL 0.3621 mL 0.9053 mL
    60 mM 0.0302 mL 0.1509 mL 0.3018 mL 0.7544 mL
    80 mM 0.0226 mL 0.1132 mL 0.2263 mL 0.5658 mL
    100 mM 0.0181 mL 0.0905 mL 0.1811 mL 0.4526 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.

    Keywords:

    Samuraciclib hydrochlorideCT7001 hydrochlorideICEC0942 hydrochlorideCDKApoptosisCyclin dependent kinaseCDK7phosphorylatesderegulationcycleAsp155PolIIanti-tumornon-covalentATP-competitivearrestInhibitorinhibitorinhibit

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    目录号：
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