Samuraciclib hydrochloride hydrate
Based on 12 publication(s) in Google Scholar
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.
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- Pureté : 99.80%
- Formule: C22H33ClN6O2
- Masse moléculaire:552.33
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Samuraciclib hydrochloride hydrate
More- Signal Transduct Target Ther. 2025 Nov 6;10(1):363. [Abstract]
- Adv Sci (Weinh). 2025 Feb;12(5):e2413103. [Abstract]
- Cell Death Dis. 2019 Aug 9;10(8):602. [Abstract]
- Clin Cancer Res. 2024 May 1;30(9):1889-1905. [Abstract]
- Proc Natl Acad Sci U S A. 2019 Jun 25;116(26):12986-12995. [Abstract]
- EMBO J. 2025 Sep 8. [Abstract]
- Int J Mol Sci. 2022 Feb 24;23(5):2493. [Abstract]
- mBio. 2025 Dec 10;16(12):e0289825. [Abstract]
- Structure. 2024 Aug 8;32(8):1040-1048.e3. [Abstract]
- J Cancer Res Clin Oncol. 2023 Jul;149(8):5255-5263. [Abstract]
- Biochem Biophys Res Commun. 2024 Nov 26:735:150608. [Abstract]
- Res Sq. 2024 Jul 29.
Customer Validation & Images
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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WB
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Cell Proliferation/Viability Assay
Activité biologique
Description
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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. Further protocols information, click here.
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Cell Line:HCT116 cells
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Concentration:0 µM, 0.1 µM, 1 µM and 10 µM
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Incubation Time:24 hours
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Result:Induced caspase 3/7 and demonstrated PARP cleavage.
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Cell Line:HCT116 cells
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Concentration:0 µM, 0.1 µM, 1 µM and 10 µM
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Incubation Time:24 hours
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Result:Showed accumulation of cells in G2/M.
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Cell Line:HCT116 cells
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Concentration:0 µM, 0.1 µM, 1 µM and 10 µM
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Incubation Time:0 hour, 4 hours, 8 hours, 16 hours or 24 hours
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Result:PolII CTD phosphorylation was inhibited in a dose and time dependent manner in HCT116 colon cancer cells.
In Vivo
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.
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Animal Model:Female nu/nu-BALB/c athymic nude mice (7-week old) with MCF7 cells[1].
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Dosage:100 mg/kg
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Administration:Oral gavage; daily; for 14 days
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Result:At day 14, tumor growth was inhibited by 60%.
Chemical Information
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Appearance Solid
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Masse moléculaire 552.33
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Formule C22H33ClN6O2
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Color White to light yellow
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SMILES
O[C@H]1CNCC[C@@H]1CNC2=NC3=C(C(C)C)C=NN3C(NCC4=CC=CC=C4)=C2.Cl.O
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Synonyms
CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (12)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
CDK7-targeted therapy effectively disrupts cell cycle progression and oncogenic signaling in head and neck cancer. [Abstract]2025 Nov 6;10(1):363. PMID: 41193441 -
Adv Sci (Weinh)
Dual Inhibition of CDK4/6 and CDK7 Suppresses Triple-Negative Breast Cancer Progression via Epigenetic Modulation of SREBP1-Regulated Cholesterol Metabolism. [Abstract]2025 Feb;12(5):e2413103. PMID: 39656925 -
Cell Death Dis
CDK7 inhibitor THZ1 inhibits MCL1 synthesis and drives cholangiocarcinoma apoptosis in combination with BCL2/BCL-XL inhibitor ABT-263. [Abstract]2019 Aug 9;10(8):602. PMID: 31399555
Samuraciclib hydrochloride hydrate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Aug 9;10(8):602. [Abstract]
HuCCT1 and HuH28 cells were treated with a novel CDK7 inhibitor Samuraciclib hydrochloride (ICEC0942) at different concentrations for 72 h. Cell viability was measured by CCK-8 assay.
Samuraciclib hydrochloride hydrate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Aug 9;10(8):602. [Abstract]
HuCCT1 and HuH28 cells were exposed to Samuraciclib hydrochloride (ICEC0942) at indicated concentrations for 24 h. RNP2, RNP2 phosphorylation and MCL1 expression were analyzed by western blotting. ICEC0942 caused a dose-dependent reduction of phosphorylation of RNP2 at S2, S5, and S7.
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Clin Cancer Res
Selective CDK7 inhibition suppresses cell cycle progression and MYC signaling while enhancing apoptosis in therapy-resistant estrogen receptor positive breast cancer. [Abstract]2024 May 1;30(9):1889-1905. PMID: 38381406
Samuraciclib hydrochloride hydrate purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2024 May 1;30(9):1889-1905. [Abstract]
Tumor growth of ER-mutant PDX1526 in presence of vehicle, fulvestrant, Samuraciclib hydrochloride (samura) (30 mg/kg; P.O.; once daily), and fulvestrant + Samuraciclib hydrochloride (Ful+samura) for 28 days (mixed modelling with Tukey multiple comparisons test). Only significant P values are denoted.
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Proc Natl Acad Sci U S A
CDK7 inhibition suppresses aberrant hedgehog pathway and overcomes resistance to smoothened antagonists. [Abstract]2019 Jun 25;116(26):12986-12995. PMID: 31182587
Samuraciclib hydrochloride hydrate purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2019 Jun 25;116(26):12986-12995. [Abstract]
Dose–response curves of Hh-driven tumor lines and control cells in response to clinical trial used CDK7i compound Samuraciclib hydrochloride (CT7001). Cells were plated in 96-well plate in triplicate and treated with CT7001 at indicated concentrations for 72 h before cell viabilities were assessed. The results showed that CT7001 exhibited more potent inhibitory effect against Hh-driven tumor lines (IC50 ranging from ∼300 to 800 nM) compared with normal control neural cells (IC50 ranging from ∼1,300 to 2,100 nM).
Samuraciclib hydrochloride hydrate purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2019 Jun 25;116(26):12986-12995. [Abstract]
Immunoblot detecting phosphorylation levels at Ser2, Ser5, Ser7 of RNAPII C-terminal domain as well as Cdk7 and total RNAPII from Hh-driven cancer cell lines treated with Samuraciclib hydrochloride (CT7001) at indicated concentrations for 8 h. An anti–β-tubulin immunoblot is shown as loading control. CT7001 treatment induced dose-dependent reduction of phosphorylation at S2, S5, and S7 of RNAPII CTD.
Samuraciclib hydrochloride hydrate purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2019 Jun 25;116(26):12986-12995. [Abstract]
qRT-PCR analysis of Gli1 and Gli2 in SmoWT-MB and SmoD477G-MB cells, as well as Gli1 in A673 and ATRT-03 cells. Cells were treated with DMSO or Samuraciclib hydrochloride (CT7001) at indicated concentrations for 8 h.
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EMBO J
Resistance to CDK7 inhibitors directed by acquired mutation of a conserved residue in cancer cells. [Abstract]2025 Sep 8. PMID: 40921851 -
Int J Mol Sci
Cyclin-Dependent Kinases (CDKs) and the Human Cytomegalovirus-Encoded CDK Ortholog pUL97 Represent Highly Attractive Targets for Synergistic Drug Combinations. [Abstract]2022 Feb 24;23(5):2493. PMID: 35269635 -
mBio
Functional insight into cyclin-dependent kinase (CDK)7 via chemical inhibition of the priority fungal pathogen Cryptococcus neoformans. [Abstract]2025 Dec 10;16(12):e0289825. PMID: 41171060 -
Structure
Protein engineering enables a soakable crystal form of human CDK7 primed for high-throughput crystallography and structure-based drug design. [Abstract]2024 Aug 8;32(8):1040-1048.e3. PMID: 38870939 -
J Cancer Res Clin Oncol
2023 Jul;149(8):5255-5263. PMID: 36401094
Samuraciclib hydrochloride hydrate purchased from MedChemExpress. Usage Cited in: J Cancer Res Clin Oncol. 2023 Jul;149(8):5255-5263. [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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Biochem Biophys Res Commun
Interaction of CDK12 with NXF1 is a new node for the linking mechanism between transcription and transportation of mRNA. [Abstract]2024 Nov 26:735:150608. PMID: 39270556 -
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Pureté et documentation
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Fiche technique (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Patel H, et al. ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment. Mol Cancer Ther. 2018 Jun;17(6):1156-1166. [Content Brief]
[2]. Hazel P, et al. Inhibitor Selectivity for Cyclin-Dependent Kinase 7: A Structural, Thermodynamic, and Modelling Study. ChemMedChem. 2017 Mar 7;12(5):372-380. [Content Brief]
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 |
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| 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 |
Samuraciclib hydrochloride hydrate Related Classifications
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