Tagarafdeg
Based on 1 Customer Validation
Tagarafdeg (CFT1946) is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC) degrader of BRAFV600E with a DC50 of 14 nM in A375 cells. Tagarafdeg is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAFV600E splice variant. Tagarafdeg can be used in tumor research.
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- Purity: 99.41%
- CAS No.: 2882165-79-7
- 화학식: C45H49F2N11O9S
- 분자량:958.00
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보관:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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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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Cereblon |
BRafV600E |
Tagarafdeg (CFT1946) (100 nM; 24 h) causes BRAFV600E degradation and inhibits MAPK Signaling with pERK loss in BRAFV600E cells but not in WT-BRAF cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A375 cells
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Concentration:100 nM
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Incubation Time:24 h
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Result:Caused BRAFV600E degradation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BRAFV600E A375 xenograft mouse model[2]
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Dosage:0.3, 3, 10 mg/kg
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Administration:PO; BID; 20 days
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Result:Shows dose-dependent tumor regression.
10 mg/kg BID dose resulted in sustained tumor regression and is the minimum efficacious dose.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2882165-79-7
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Appearance Solid
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분자량 958.00
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화학식 C45H49F2N11O9S
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Color Off-white to light yellow
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SMILES
CN1C(C(C(N(CCC2=O)C(N2)=O)=N1)=C3)=CC(N(CC4)CCC4(O)CC(N5CCC6(C[C@@H](N(C=NC7=CC=C8OC(C(F)=CC=C9N[S](N(C)CC)(=O)=O)=C9C#N)C(C7=C8)=O)CO6)CC5)=O)=C3F
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Synonyms
CFT1946
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
용액&용해도
DMSO : 100 mg/mL (104.38 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)
순도&문서
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Data Sheet (272 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 1.0438 mL | 5.2192 mL | 10.4384 mL | 26.0960 mL |
| 5 mM | 0.2088 mL | 1.0438 mL | 2.0877 mL | 5.2192 mL | |
| 10 mM | 0.1044 mL | 0.5219 mL | 1.0438 mL | 2.6096 mL | |
| 15 mM | 0.0696 mL | 0.3479 mL | 0.6959 mL | 1.7397 mL | |
| 20 mM | 0.0522 mL | 0.2610 mL | 0.5219 mL | 1.3048 mL | |
| 25 mM | 0.0418 mL | 0.2088 mL | 0.4175 mL | 1.0438 mL | |
| 30 mM | 0.0348 mL | 0.1740 mL | 0.3479 mL | 0.8699 mL | |
| 40 mM | 0.0261 mL | 0.1305 mL | 0.2610 mL | 0.6524 mL | |
| 50 mM | 0.0209 mL | 0.1044 mL | 0.2088 mL | 0.5219 mL | |
| 60 mM | 0.0174 mL | 0.0870 mL | 0.1740 mL | 0.4349 mL | |
| 80 mM | 0.0130 mL | 0.0652 mL | 0.1305 mL | 0.3262 mL | |
| 100 mM | 0.0104 mL | 0.0522 mL | 0.1044 mL | 0.2610 mL |
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