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Samuraciclib

(別名: CT7001; ICEC0942)
12 Cited Publications
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Based on 12 publication(s) in Google Scholar

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

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  • 純度: 99.55%
  • CAS 番号: 1805833-75-3
  • 分子式: C22H30N6O
  • 分子量:394.51
  • 保管条件:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 6 months , -20°C, 1 month
  • Samuraciclib Chemical Structure
    Samuraciclib 構造式
  • Experimental Validation Results for Samuraciclib
  • Experimental Validation Results for Samuraciclib
  • Experimental Validation Results for Samuraciclib
  • Experimental Validation Results for Samuraciclib
  • Experimental Validation Results for Samuraciclib
  • Experimental Validation Results for Samuraciclib
  • Experimental Validation Results for Samuraciclib
CAS 番号: 1805833-75-3
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  • Samuraciclib Chemical Structure
    Samuraciclib Chemical Structure
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  • 1/16

    Samuraciclib purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2024 May 1;30(9):1889-1905. [Abstract]

    Customer Validation
     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.

  • 1/16

    Samuraciclib purchased from MedChemExpress. Usage Cited in: J Cancer Res Clin Oncol. 2023 Jul;149(8):5255-5263. [Abstract]

    Customer Validation
     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).

  • 1/16

    Samuraciclib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Aug 9;10(8):602. [Abstract]

    Customer Validation
     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.

  • 1/16

    Samuraciclib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Aug 9;10(8):602. [Abstract]

    Customer Validation
     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.

  • 1/16

    Samuraciclib purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2019 Jun 25;116(26):12986-12995. [Abstract]

    Customer Validation
     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).

  • 1/16

    Samuraciclib purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2019 Jun 25;116(26):12986-12995. [Abstract]

    Customer Validation
     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.

  • 1/16

    Samuraciclib purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2019 Jun 25;116(26):12986-12995. [Abstract]

    Customer Validation
     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.

  • Samuraciclib