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: 99.88%
COA Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 365 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 365 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 490 In-stock
Estimated Time of Arrival: December 31
25 mg USD 980 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1600 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Samuraciclib hydrochloride hydrate:

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).

    View All CDK Isoform Specific Products:

    View All Isoforms
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK

    • 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/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].

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

    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].

    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

    Appearance

    Solid

    Formula

    C22H33ClN6O2
    SMILES

    O[[email protected]]1CNCC[[email protected]@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)

    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
    10 mM 0.1811 mL 0.9053 mL 1.8105 mL
    *Please refer to the solubility information to select the appropriate solvent.
    Purity & Documentation
    References
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    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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    Keywords:

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

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