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-103712C Purity: 98.60%
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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 365 In-stock
Solution
10 mM * 1 mL in DMSO USD 365 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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    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/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)

    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].

    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, 0.1 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) 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].

    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

    552.33

    Formula

    C22H33ClN6O2
    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.Cl.O.[2.5].[3.7]
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (181.05 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 1.8105 mL 9.0526 mL 18.1051 mL
    5 mM 0.3621 mL 1.8105 mL 3.6210 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 (sealed storage, 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)

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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 Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    (per animal)

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    (per animal)

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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
    Purity & Documentation

    Purity: 99.88%

    COA (254 KB) HNMR (303 KB) LCMS (293 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 (sealed storage, 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 1.8105 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
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    Samuraciclib hydrochloride hydrate 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:

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

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