FRC-222
Based on 1 Customer Validation
FRC-222 is a CHD1 tandem chromodomain inhibitor with a Kd of 0.15 μM and an IC50 of 0.18 μM. FRC-222 binds to the H3K4me3 binding site of CHD1 tandem chromodomain via aromatic cage interactions and extended ligand contacts. FRC-222 can be used for the research of prostate cancer[1].
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.30%
- Fòrmula: C36H45N5O2
- Peso molecular:579.77
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Actividad biológica
Descripciòn
In Vitro
FRC-222 (Compound 2n) binds to purified recombinant CHD1 tandem chromodomain with a Kd of 0.15 μM[1].
FRC-222 inhibits the interaction between purified recombinant CHD1 tandem chromodomain and H3K4me3 peptide with an IC50 of 0.49 μM[1].
FRC-222 (25-100 μM) engages endogenous full-length CHD1 in HEK293T cell lysate, competitively inhibiting its binding to LSD1-K114me3 peptide in a concentration-dependent manner[1].
FRC-222 (10 μM) shows high selectivity against purified LSD1, KMT9, METTL21A, EHMT2 (G9a), SET8, and NSD2 enzymes, with minimal inhibition of DNMT1[1].
FRC-222 (16 μM) shows high selectivity against purified TAF3, SPIN1, and PHF8 methyl-lysine reader domains, with no significant inhibition of H3K4me3 peptide binding[1].
FRC-222 (0.8-6 μM; 48 h) impairs the viability of PC-3M-Luc prostate cancer cells in a concentration-dependent manner, with significant inhibition observed at concentrations ≥1.8 μM[1].
FRC-222 (0.8-6 μM; 48 h) potently impairs the viability of 22Rv1 prostate cancer cells in a concentration-dependent manner, with significant inhibition observed at concentrations ≥1.8 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC-3M-Luc prostate cancer cells
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Concentration:0.8 μM; 1.2 μM; 1.8 μM; 2.7 μM; 4 μM; 6 μM
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Incubation Time:48 h
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Result:Retained over 110% of control cell viability at 0.8 μM and 1.2 μM.
Reduced viability to 60% of control at 1.8 μM.
Reduced viability to 35% of control at 2.7 μM.
Reduced viability to 25% of control at 4 μM.
Reduced viability to ~5% of control at 6 μM.
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Cell Line:22Rv1 prostate cancer cells
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Concentration:0.8 μM; 1.2 μM; 1.8 μM; 2.7 μM; 4 μM; 6 μM
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Incubation Time:48 h
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Result:Retained over 110% of control cell viability at 0.8 μM.
Retained ~90% of control viability at 1.2 μM.
Reduced viability to ~10% of control at 1.8 μM.
Reduced viability to ≤10% of control at concentrations ≥2.7 μM.
Chemical Information
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Appearance Solid
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Peso molecular 579.77
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Fòrmula C36H45N5O2
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Color White to off-white
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SMILES
COC1=CC=C(C=C1)CNC2CCN(C3=NC4=CC(OCC)=CC=C4C(NC5CCN(CC6=CC=CC=C6)CC5)=C3)CC2
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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 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (172.48 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. 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. 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)
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 (4.31 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 (4.31 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 (273 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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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, 6 months; -20°C, 1 month. 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 | 1.7248 mL | 8.6241 mL | 17.2482 mL | 43.1205 mL |
| 5 mM | 0.3450 mL | 1.7248 mL | 3.4496 mL | 8.6241 mL | |
| 10 mM | 0.1725 mL | 0.8624 mL | 1.7248 mL | 4.3121 mL | |
| 15 mM | 0.1150 mL | 0.5749 mL | 1.1499 mL | 2.8747 mL | |
| 20 mM | 0.0862 mL | 0.4312 mL | 0.8624 mL | 2.1560 mL | |
| 25 mM | 0.0690 mL | 0.3450 mL | 0.6899 mL | 1.7248 mL | |
| 30 mM | 0.0575 mL | 0.2875 mL | 0.5749 mL | 1.4374 mL | |
| 40 mM | 0.0431 mL | 0.2156 mL | 0.4312 mL | 1.0780 mL | |
| 50 mM | 0.0345 mL | 0.1725 mL | 0.3450 mL | 0.8624 mL | |
| 60 mM | 0.0287 mL | 0.1437 mL | 0.2875 mL | 0.7187 mL | |
| 80 mM | 0.0216 mL | 0.1078 mL | 0.2156 mL | 0.5390 mL | |
| 100 mM | 0.0172 mL | 0.0862 mL | 0.1725 mL | 0.4312 mL |
FRC-222 Related Classifications
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