TCIP3
Based on 1 Customer Validation
TCIP3 is a bivalent molecular glue degrader that binds dually to p300/CBP and BCL6. TCIP3 redirects p300 and CBP, thereby activating programmed cell death genes that are normally repressed by the oncogenic driver gene BCL6. TCIP3 induces acetylation of BCL6 and histone tails, inhibits c-MYC transcription. TCIP3 can be used for the research of diffuse large B-cell lymphoma (DLBCL).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.30%
- No. CAS: 3067681-36-8
- Fòrmula: C58H71ClF2N16O7
- Peso molecular:1177.74
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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
Actividad biológica
Descripciòn
In Vitro
TCIP3 (1-10 nM; 1-24 h) mediates rapid, potent, and ternary complex-dependent c-MYC inhibition in SUDHL5 cells; in lymphoma and leukemia cell lines, the degree of c-MYC inhibition correlates directly with BCL6 expression levels, while this inhibitory effect is significantly attenuated in cell lines with c-MYC chromosomal rearrangement[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SUDHL5, K422, DB, DAUDI, OCILY19, TOLEDO, K562, RAJI
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Concentration:1 nM; 10 nM (co-treated with 500 nM BI-3812 (HY-111381) or 500 nM GNE-781 (HY-108696))
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Incubation Time:1 h; 2 h; 4 h; up to 24 h
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Result:Reduced c-MYC mRNA half-life to 33 minutes in SUDHL5 cells, with repression persisting over 24 hours.
Reduced c-MYC protein half-life to 2.5 hours, with an IC50 of 0.8 nM for repression at 4 hours.
Restored c-MYC levels to baseline or inhibitor-only levels when co-treated with BI-3812 or GNE-781.
Showed more pronounced c-MYC repression in high-BCL6 cell lines (SUDHL5, K422, DB, DAUDI).
Showed muted c-MYC repression in cell lines with c-MYC chromosomal rearrangements (DB, DAUDI, RAJI).
Chemical Information
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No. CAS 3067681-36-8
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Appearance Solid
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Peso molecular 1177.74
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Fòrmula C58H71ClF2N16O7
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Color White to off-white
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SMILES
O=C(N1CC2=C(CC1)N(C3CCN(CC3)C(CCN4CCN(CC4)C(C5CCN(CC5)C6=NC=C(C(NC7=CC(C=C(C(N8C)=O)OCC(NC)=O)=C8C(OC)=C7)=N6)Cl)=O)=O)N=C2N9C%10=C(CCC9)C=C(C%11=CN(C)N=C%11)C(C(F)F)=C%10)NC
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Synonyms
KAT-TCIP
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (84.91 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 (protect from light). 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 (protect from light). 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (protect from light). 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 | 0.8491 mL | 4.2454 mL | 8.4908 mL | 21.2271 mL |
| 5 mM | 0.1698 mL | 0.8491 mL | 1.6982 mL | 4.2454 mL | |
| 10 mM | 0.0849 mL | 0.4245 mL | 0.8491 mL | 2.1227 mL | |
| 15 mM | 0.0566 mL | 0.2830 mL | 0.5661 mL | 1.4151 mL | |
| 20 mM | 0.0425 mL | 0.2123 mL | 0.4245 mL | 1.0614 mL | |
| 25 mM | 0.0340 mL | 0.1698 mL | 0.3396 mL | 0.8491 mL | |
| 30 mM | 0.0283 mL | 0.1415 mL | 0.2830 mL | 0.7076 mL | |
| 40 mM | 0.0212 mL | 0.1061 mL | 0.2123 mL | 0.5307 mL | |
| 50 mM | 0.0170 mL | 0.0849 mL | 0.1698 mL | 0.4245 mL | |
| 60 mM | 0.0142 mL | 0.0708 mL | 0.1415 mL | 0.3538 mL | |
| 80 mM | 0.0106 mL | 0.0531 mL | 0.1061 mL | 0.2653 mL |
TCIP3 Related Classifications
HY-173552 Related Classifications
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