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

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

Cat. No.: HY-103712B
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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.

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

Samuraciclib hydrochloride hydrate Chemical Structure

Samuraciclib hydrochloride hydrate Chemical Structure

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 333 In-stock
Solution
10 mM * 1 mL in DMSO USD 333 In-stock
Solid
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
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Samuraciclib hydrochloride hydrate:

Samuraciclib hydrochloride hydrate Related Antibodies

Top Publications Citing Use of Products

    Samuraciclib hydrochloride hydrate 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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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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

    41 nM (IC50)

    CDK2

    578 nM (IC50)

    CDK1

    1.8 μM (IC50)

    CDK4

    49 μM (IC50)

    CDK5

    9.4 μM (IC50)

    CDK6

    31 μM (IC50)

    CDK9

    1.2 μM (IC50)

    In Vitro

    Samuraciclib hydrochloride hydrate (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment promotes cell apoptosis[1].
    Samuraciclib hydrochloride hydrate (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment induces cell cycle arrest[1].
    Samuraciclib hydrochloride hydrate (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. Samuraciclib trihydrochloride 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].

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

    Samuraciclib hydrochloride hydrate 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, 0.01 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) 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) hydrochloride hydrate 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

    521.70

    Formula

    C22H30N6O.(2.5HCl).(2H2O)
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O[C@H]1CNCC[C@@H]1CNC2=NC3=C(C(C)C)C=NN3C(NCC4=CC=CC=C4)=C2.Cl.O.O.[2.5]
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, stored under nitrogen, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (191.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9168 mL 9.5841 mL 19.1681 mL
    5 mM 0.3834 mL 1.9168 mL 3.8336 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, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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 (4.79 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 (4.79 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.08%

    COA (255 KB) HNMR (283 KB) LCMS (259 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, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9168 mL 9.5841 mL 19.1681 mL 47.9203 mL
    5 mM 0.3834 mL 1.9168 mL 3.8336 mL 9.5841 mL
    10 mM 0.1917 mL 0.9584 mL 1.9168 mL 4.7920 mL
    15 mM 0.1278 mL 0.6389 mL 1.2779 mL 3.1947 mL
    20 mM 0.0958 mL 0.4792 mL 0.9584 mL 2.3960 mL
    25 mM 0.0767 mL 0.3834 mL 0.7667 mL 1.9168 mL
    30 mM 0.0639 mL 0.3195 mL 0.6389 mL 1.5973 mL
    40 mM 0.0479 mL 0.2396 mL 0.4792 mL 1.1980 mL
    50 mM 0.0383 mL 0.1917 mL 0.3834 mL 0.9584 mL
    60 mM 0.0319 mL 0.1597 mL 0.3195 mL 0.7987 mL
    80 mM 0.0240 mL 0.1198 mL 0.2396 mL 0.5990 mL
    100 mM 0.0192 mL 0.0958 mL 0.1917 mL 0.4792 mL
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    Samuraciclib hydrochloride hydrate Related Classifications

    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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