Samuraciclib

• UNSPSC Description:

  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[1][2].

• Target Antigen:

  Apoptosis; CDK

• Type:

  Reference compound

• Related Pathways:

  Apoptosis;Cell Cycle/DNA Damage

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/samuraciclib.html

• Solubility:

  10 mM in DMSO

• Smiles:

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

• Molecular Weight:

  394.51

• References & Citations:

  [1]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.|[2]Patel H, et al. ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment. Mol Cancer Ther. 2018 Jun;17(6):1156-1166.Int J Mol Sci. 2022 Feb 24;23(5):2493.|J Cancer Res Clin Oncol. 2022 Nov 18.|Biochem Biophys Res Commun. 2024 Aug 28:735:150608.|Cell Death Dis. 2019 Aug 9;10(8):602.|Clin Cancer Res. 2024 Feb 21.|Proc Natl Acad Sci U S A. 2019 Jun 25;116(26):12986-12995. |Res Sq. 2024 Jul 29.|Structure. 2024 Jun 9:S0969-2126(24)00188-6.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  Phase 2

• CAS Number:

  1805833-75-3