CFT-1297
Based on 1 Customer Validation
CFT-1297 is a CRBN-recruiting BRD4 PROTAC degrader with a DC50 of 5 nM; it has KD values of 2.1 μM, 0.68 μM and 58 nM for CRBN, BRD4 (BD2) and BRD4 (BD1), respectively. CFT-1297 binds weakly to CRBN-DDB1, with a KD value of 2.1 μM.
(Pink: BRD4 ligand (HY-132942); Blue: Cereblon ligand (HY-A0003); Black: linker).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 96.06%
- CAS No.: 2154353-03-2
- 화학식: C47H50ClN9O3
- 분자량:824.41
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보관:Powder -20°C, 3 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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
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BRD4 5 nM (DC50) |
BRD4 (BD1) 58 nM (Kd) |
BRD4 (BD2) 0.68 μM (Kd) |
Cereblon 2.1 μM (Kd) |
CFT-1297 (3 h) degrades full-length BRD4 in HEK293T cells with a DC50 of 5 nM and reduces protein levels to an Emax of 3% after 3 h[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2154353-03-2
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Appearance Solid
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분자량 824.41
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화학식 C47H50ClN9O3
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Color White to off-white
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SMILES
CC1=NN=C2N1C3=C(C(C4=CC=C(C=C4)Cl)=NC25CC5)C=C(C=C3)C6=CN(N=C6)CCCCCCCN7CCC(CC7)C8=CC=CC9=C8CN(C9=O)C%10CCC(NC%10=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (121.30 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)
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 (3.03 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.
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.
순도&문서
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Kroupova A, et al. Design of a Cereblon construct for crystallographic and biophysical studies of protein degraders. Nature communications. 2024 Oct 15;15(1):8885. [Content Brief]
[2]. Eron SJ, et al. Structural Characterization of Degrader-Induced Ternary Complexes Using Hydrogen-Deuterium Exchange Mass Spectrometry and Computational Modeling: Implications for Structure-Based Design. ACS chemical biology. 2021 Nov 19;16(11):2228-2243. [Content Brief]
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 | 1.2130 mL | 6.0649 mL | 12.1299 mL | 30.3247 mL |
| 5 mM | 0.2426 mL | 1.2130 mL | 2.4260 mL | 6.0649 mL | |
| 10 mM | 0.1213 mL | 0.6065 mL | 1.2130 mL | 3.0325 mL | |
| 15 mM | 0.0809 mL | 0.4043 mL | 0.8087 mL | 2.0216 mL | |
| 20 mM | 0.0606 mL | 0.3032 mL | 0.6065 mL | 1.5162 mL | |
| 25 mM | 0.0485 mL | 0.2426 mL | 0.4852 mL | 1.2130 mL | |
| 30 mM | 0.0404 mL | 0.2022 mL | 0.4043 mL | 1.0108 mL | |
| 40 mM | 0.0303 mL | 0.1516 mL | 0.3032 mL | 0.7581 mL | |
| 50 mM | 0.0243 mL | 0.1213 mL | 0.2426 mL | 0.6065 mL | |
| 60 mM | 0.0202 mL | 0.1011 mL | 0.2022 mL | 0.5054 mL | |
| 80 mM | 0.0152 mL | 0.0758 mL | 0.1516 mL | 0.3791 mL | |
| 100 mM | 0.0121 mL | 0.0606 mL | 0.1213 mL | 0.3032 mL |
CFT-1297 Related Classifications
HY-168546 Related Classifications
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