Fadraciclib
Based on 6 publication(s) in Google Scholar
Fadraciclib (CYC065) is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50s of 5 and 26 nM, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.77%
- No. CAS: 1070790-89-4
- Fòrmula: C21H31N7O
- Peso molecular:397.52
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Fadraciclib
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Cell Imaging/Staining
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
CDK2 |
CDK9 |
In Vitro
Fadraciclib blocks cells in the G1 phase of the cell cycle and inhibits cell growth specifically in cyclin E1 (CCNE1)-overexpressing uterine serous carcinomas (USCs). USC cell lines expressing high CCNE1 mRNA and protein levels to be significantly more sensitive to treatment with Fadraciclib in vitro when compared with low CCNE1-expressing cell lines (IC50: mean±s.d.=124.1±57.8 nM in CCNE1-overexpressing USC cell lines vs 415±117.5 nM in CCNE1 low expressors, respectively; P=0.0003). Importantly, low concentrations of Fadraciclib (i.e., 100 nM) causes an arrest in the G1 phase of the cell cycle only in the CCNE1-overexpressing USC cell lines (i.e., USC-ARK-2, USC-ARK-7) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1070790-89-4
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Appearance Solid
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Peso molecular 397.52
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Fòrmula C21H31N7O
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Color White to off-white
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SMILES
C[C@@H](O)[C@@H](NC1=NC(NCC2=C(C)C=C(C)N=C2)=C3N=CN(C(C)C)C3=N1)CC
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Synonyms
CYC065
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell
2023 Jun 8;186(12):2628-2643.e21. PMID: 37267950
Fadraciclib purchased from MedChemExpress. Usage Cited in: Cell. 2023 Jun 8;186(12):2628-2643.e21. [Abstract]
Gliomasphere morphology and viability was followed using Calcein-AM staining 72 h post-treatment with DMSO control, 3 μM CYC065 (Fadraciclib) and 100 nM THZ1 in primary gliomasphere culture-N15-0661.
Fadraciclib purchased from MedChemExpress. Usage Cited in: Cell. 2023 Jun 8;186(12):2628-2643.e21. [Abstract]
Gliomasphere morphology and viability was followed using Calcein-AM staining 72 h post-treatment with DMSO control, 3 μM CYC065 (Fadraciclib) and 100 nM THZ1 in recurrent gliomasphere culture—GTCC-9.
Fadraciclib purchased from MedChemExpress. Usage Cited in: Cell. 2023 Jun 8;186(12):2628-2643.e21. [Abstract]
Cell viability was measured 72 h post-treatment with increasing concentrations of CYC065 (Fadraciclib, 1-10 μ M) and THZ1 in patient-derived gliomaspheres using WST-1 viability assay.
Fadraciclib purchased from MedChemExpress. Usage Cited in: Cell. 2023 Jun 8;186(12):2628-2643.e21. [Abstract]
Cell viability was determined using WST-1 viability assays in mouse primary cortical neurons 96 h post-treatment with increasing concentrations of CYC065 (Fadraciclib, 1-10 μ M) and THZ1.
Fadraciclib purchased from MedChemExpress. Usage Cited in: Cell. 2023 Jun 8;186(12):2628-2643.e21. [Abstract]
Western blot analysis of whole-cell lysates collected 72 h post-treatment with DMSO, 3 μM CYC065 (Fadraciclib) or 100 nM THZ1 in N16-0125 and N15-0385 gliomaspheres.
Fadraciclib purchased from MedChemExpress. Usage Cited in: Cell. 2023 Jun 8;186(12):2628-2643.e21. [Abstract]
Flow cytometry using AnnexinV/PI staining was employed to assess the number of AnnexinV+/PI+ cells following 72 h treatment with DMSO, 3 μM CYC065 (Fadraciclib) or 100 nM THZ1 in N15-1027 and N14-1208 gliomaspheres.
Fadraciclib purchased from MedChemExpress. Usage Cited in: Cell. 2023 Jun 8;186(12):2628-2643.e21. [Abstract]
Levels of Mcl-1, cleaved caspase-3, RNAPII CTD Ser2/5 phosphorylation and RNAPII in the gliomaspheres upon treatment with DMSO, 3 μM CYC065 (Fadraciclib) or 100 nM THZ1 for 72 h were followed using Western blot analysis.
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Cell Death Dis
Transcriptional CDK inhibitors, CYC065 and THZ1 promote Bim-dependent apoptosis in primary and recurrent GBM through cell cycle arrest and Mcl-1 downregulation. [Abstract]2021 Aug 3;12(8):763. PMID: 34344865 -
NPJ Precis Oncol
Co-targeting CDK2 and CDK4/6 overcomes resistance to aromatase and CDK4/6 inhibitors in ER+ breast cancer. [Abstract]2022 Sep 24;6(1):68. PMID: 36153348 -
Cells
Transcriptional CDK Inhibitors CYC065 and THZ1 Induce Apoptosis in Glioma Stem Cells Derived from Recurrent GBM. [Abstract]2021 May 12;10(5):1182. PMID: 34066147 -
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 -
Solvente y solubilidad
In Vitro:
DMSO : ≥ 100 mg/mL (251.56 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5156 mL | 12.5780 mL | 25.1560 mL | 62.8899 mL |
| 5 mM | 0.5031 mL | 2.5156 mL | 5.0312 mL | 12.5780 mL | |
| 10 mM | 0.2516 mL | 1.2578 mL | 2.5156 mL | 6.2890 mL | |
| 15 mM | 0.1677 mL | 0.8385 mL | 1.6771 mL | 4.1927 mL | |
| 20 mM | 0.1258 mL | 0.6289 mL | 1.2578 mL | 3.1445 mL | |
| 25 mM | 0.1006 mL | 0.5031 mL | 1.0062 mL | 2.5156 mL | |
| 30 mM | 0.0839 mL | 0.4193 mL | 0.8385 mL | 2.0963 mL | |
| 40 mM | 0.0629 mL | 0.3144 mL | 0.6289 mL | 1.5722 mL | |
| 50 mM | 0.0503 mL | 0.2516 mL | 0.5031 mL | 1.2578 mL | |
| 60 mM | 0.0419 mL | 0.2096 mL | 0.4193 mL | 1.0482 mL | |
| 80 mM | 0.0314 mL | 0.1572 mL | 0.3144 mL | 0.7861 mL | |
| 100 mM | 0.0252 mL | 0.1258 mL | 0.2516 mL | 0.6289 mL |
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