Tagarafdeg
Based on 1 publication(s) in Google Scholar
Tagarafdeg (CFT1946) is an orally active, blood-brain barrier-penetrant, and selective bifunctional BiDAC degrader of the BRAFV600E/K mutant protein, with a DC50 of 14 nM in A375 cells. Tagarafdeg mediates the ubiquitination and proteasomal degradation of BRAF mutant proteins. Tagarafdeg inhibits tumor progression in multiple models of BRAFV600E-mutant intracranial tumors, melanoma, and colorectal cancer. Tagarafdeg is applicable to tumor-related research.
(Pink: Braf ligand (HY-187012); Blue: Cereblon ligand (HY-49385); Black: linker).
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- Pureza : 99.41%
- No. CAS: 2882165-79-7
- Fòrmula: C45H49F2N11O9S
- Peso molecular:958.00
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Almacenamiento:
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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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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Publications Citing Use of MedChemExpress (MCE) Tagarafdeg
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
BRafV600E 14 nM (DC50) |
In Vitro
Tagarafdeg (CFT1946) (1-10000 nM; 24 h) degrades BRAFV600E protein and downregulates pERK protein levels in a dose-dependent manner in A375 cells (DC50 = 14 nM, Emax = 26%); it does not degrade wild-type BRAF protein in HCT116 cells harboring wild-type BRAF, and exerts almost no effect on the MAPK signaling pathway and cell proliferation[1].
Tagarafdeg inhibits the proliferation of BRAF inhibitor-resistant A375‑NRAS Q61K cells (GI50 = 150 nM); it exhibits weak antiproliferative activity against HepG2 cells (GI50 >10 μM)[1].
Tagarafdeg (100 nM; 24 h) induces the degradation of BRAFV600E and inhibits MAPK signal transduction, resulting in the loss of pERK in BRAFV600E cells, but exerts no effect in WTV600E cells[1].
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
co‑treatment with 10 μM competing ligand (targeting ligand / CRBN ligand / MLN4924 (HY-70062) / Bortezomib (HY-10227)) -
Incubation Time:24 h
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Result:Abolished CFT1946‑mediated BRAF‑V600E degradation via target‑ligand competition, CRBN‑ligand competition, CUL4‑E3 inhibition and proteasome inhibition.
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Cell Line:A375 cells
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Concentration:1, 10, 100, 1000, 10000 nM
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Incubation Time:24 h
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Result:Induced dose‑dependent BRAF‑V600E degradation and reduced pERK levels; the CRBN‑binding‑deficient analogue CFT1946NMe failed to degrade BRAF‑V600E.
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Cell Line:HCT116 cells
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Concentration:1, 10, 100, 1000, 10000 nM
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Incubation Time:24 h
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Result:Exerted no obvious alterations on protein abundance of WT‑BRAF, pERK and total‑ERK.
In Vivo
Tagarafdeg (10-30 mg/kg; oral administration, twice daily) inhibits tumor growth in BRAF inhibitor-resistant A375-NRAS Q61K xenograft mice, and its combination with the MEK inhibitor Trametinib (HY-10999) yields an enhanced antitumor effect[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2882165-79-7
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Appearance Solid
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Peso molecular 958.00
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
Solvente y solubilidad
In Vitro:
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)
Pureza y Documentación
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Ficha de datos (283 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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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, 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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