CFT8634
Based on 1 publication(s) in Google Scholar
CFT8634 is an orally bioavailable PROTAC BRD9 targeted degrader based on the E3 ubiquitin ligase CRBN mechanism. CFT8634 can be used for the study of synovial sarcoma and SMARCB1-deficient solid tumors (Pink: BRD9 ligand (HY-169988); Blue: E3 ligase ligand (HY-169989); Black: linker (HY-169991). CFT8634 is a heterobifunctional molecule that binds to BRD9 at one end and recruits CRBN at the other end, which can inhibit the growth of tumor cells that depend on BRD9. CFT8634 can be used for the study of SMARCB1-related cancers (such as synovial sarcoma and malignant rhabdoid tumor).
(Pink: BRD9 ligand (HY-169988); Blue: Cereblon ligand (HY-169989); Black: linker (HY-169991)).
For research use only. We do not sell to patients.
- Purity: 98.10%
- CAS No.: 2704617-96-7
- Formula: C37H45F3N6O5
- Molecular Weight:710.79
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications Citing Use of MedChemExpress (MCE) CFT8634
MoreAll PROTACs Isoforms
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Biological Activity
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Cereblon |
BRD9 |
CFT8634 (compound 18) degrades BRD9 in synovial sarcoma and malignant rhabdoid tumor cell lines and has a DC50 of 2.7 nM for SMARCB-1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2704617-96-7
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Appearance Solid
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Molecular Weight 710.79
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Formula C37H45F3N6O5
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Color Light green to gray
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SMILES
CC(C(C1=CC(OC)=C(C(OC)=C1)CN2CC(F)([C@@H](N3CCN(C4=C(C=C(C=C4)N[C@@H]5C(NC(CC5)=O)=O)F)CC3)CC2)F)=CN6C)=C(C)C6=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : 100 mg/mL (140.69 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, stored under nitrogen). 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, stored under nitrogen). 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 (3.52 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 (3.52 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.
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, stored under nitrogen)
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.
Purity & Documentation
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Data Sheet (272 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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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, stored under nitrogen). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4069 mL | 7.0344 mL | 14.0689 mL | 35.1721 mL |
| 5 mM | 0.2814 mL | 1.4069 mL | 2.8138 mL | 7.0344 mL | |
| 10 mM | 0.1407 mL | 0.7034 mL | 1.4069 mL | 3.5172 mL | |
| 15 mM | 0.0938 mL | 0.4690 mL | 0.9379 mL | 2.3448 mL | |
| 20 mM | 0.0703 mL | 0.3517 mL | 0.7034 mL | 1.7586 mL | |
| 25 mM | 0.0563 mL | 0.2814 mL | 0.5628 mL | 1.4069 mL | |
| 30 mM | 0.0469 mL | 0.2345 mL | 0.4690 mL | 1.1724 mL | |
| 40 mM | 0.0352 mL | 0.1759 mL | 0.3517 mL | 0.8793 mL | |
| 50 mM | 0.0281 mL | 0.1407 mL | 0.2814 mL | 0.7034 mL | |
| 60 mM | 0.0234 mL | 0.1172 mL | 0.2345 mL | 0.5862 mL | |
| 80 mM | 0.0176 mL | 0.0879 mL | 0.1759 mL | 0.4397 mL | |
| 100 mM | 0.0141 mL | 0.0703 mL | 0.1407 mL | 0.3517 mL |