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

Samuraciclib hydrochloride  (Synonyms: CT7001 hydrochloride; ICEC0942 hydrochloride)

Cat. No.: HY-103712A Purity: 98.80%
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Samuraciclib hydrochloride (CT7001 hydrochloride; ICEC0942 hydrochloride) est un inhibiteur de CDK7 qui est puissant, sélectif, ATP-compétitif et oralement actif, avec un IC50 de 41 nM. Samuraciclib hydrochloride présente une sélectivité de 45, 15, 230 et 30 fois sur CDK1, CDK2 (IC50 de 578 nM), CDK5 et CDK9, respectivement. Samuraciclib hydrochloride inhibe la croissance des lignées cellulaires du cancer du sein avec des valeurs GI50 entre 0,2 et 0,3 µM. Samuraciclib hydrochloride a des effets anti-tumoraux.

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

For research use only. We do not sell to patients.

Samuraciclib hydrochloride Chemical Structure

Samuraciclib hydrochloride Chemical Structure

CAS No. : 1805789-54-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 330 In-stock
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Solid
1 mg USD 142 In-stock
5 mg USD 300 In-stock
10 mg USD 490 In-stock
25 mg USD 980 In-stock
50 mg USD 1600 In-stock
100 mg USD 2500 In-stock
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Based on 6 publication(s) in Google Scholar

Other Forms of Samuraciclib hydrochloride:

Samuraciclib hydrochloride Related Antibodies

Top Publications Citing Use of Products

    Samuraciclib hydrochloride purchased from MedChemExpress. 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).

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    Description

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

    IC50 & Target[1][2]

    CDK7

    41 nM (IC50)

    CDK2

    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)

    In Vitro

    Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment promotes cell apoptosis[1].
    ? Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment induces cell cycle arrest[1].
    ? Samuraciclib (ICEC0942; 0-10 μM; 0-24 hours; HCT116 cells) treatment inhibits the phosphorylation of PolII CTD in a dose and time dependent manner in HCT116 colon cancer cells. ICEC0942 also inhibits phosphorylation of CDK1, CDK2 and retinoblastoma[1].
    ? Samuraciclib (ICEC0942) 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].

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

    Samuraciclib hydrochloride Related Antibodies

    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, 0.01 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.
    In Vivo

    Samuraciclib (ICEC0942; 100 mg/kg; oral gavage; daily; for 14 days; female nu/nu-BALB/c athymic nude mice) 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].

    MedChemExpress (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
    Molecular Weight

    430.97

    Formula

    C22H31ClN6O
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O[C@H]1CNCC[C@@H]1CNC2=NC3=C(C(C)C)C=NN3C(NCC4=CC=CC=C4)=C2.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, stored under nitrogen, away from moisture

    *In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (232.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 55 mg/mL (127.62 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3203 mL 11.6017 mL 23.2035 mL
    5 mM 0.4641 mL 2.3203 mL 4.6407 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 100 mg/mL (232.03 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.98%

    COA (253 KB) HNMR (213 KB) LCMS (466 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.3203 mL 11.6017 mL 23.2035 mL 58.0087 mL
    5 mM 0.4641 mL 2.3203 mL 4.6407 mL 11.6017 mL
    10 mM 0.2320 mL 1.1602 mL 2.3203 mL 5.8009 mL
    15 mM 0.1547 mL 0.7734 mL 1.5469 mL 3.8672 mL
    20 mM 0.1160 mL 0.5801 mL 1.1602 mL 2.9004 mL
    25 mM 0.0928 mL 0.4641 mL 0.9281 mL 2.3203 mL
    30 mM 0.0773 mL 0.3867 mL 0.7734 mL 1.9336 mL
    40 mM 0.0580 mL 0.2900 mL 0.5801 mL 1.4502 mL
    50 mM 0.0464 mL 0.2320 mL 0.4641 mL 1.1602 mL
    60 mM 0.0387 mL 0.1934 mL 0.3867 mL 0.9668 mL
    80 mM 0.0290 mL 0.1450 mL 0.2900 mL 0.7251 mL
    100 mM 0.0232 mL 0.1160 mL 0.2320 mL 0.5801 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Samuraciclib hydrochloride Related Classifications

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    • 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:

    Samuraciclib1805789-54-1CT7001ICEC0942CT 7001CT-7001ICEC 0942ICEC-0942CDKApoptosisCyclin dependent kinaseCDK7phosphorylatesderegulationcycleAsp155PolIIanti-tumornon-covalentATP-competitivearrestInhibitorinhibitorinhibit

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