2882165-79-7
Chemical Structure
Tagarafdeg
Synonym(s): CFT1946
- CAS No.: 2882165-79-7
- Formula:C45H49F2N11O9S
- Molecular Weight:958.00
InChIKey: OCDRMYDQTIPVOI-HHHXNRCGSA-N
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
Biological Activity: 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[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
Tagarafdeg | 99.41% | 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. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Yanke Liang. The Discovery and Characterization of CFT1946: A Potent, Selective, and Orally Bioavailable Degrader of Mutant BRAF for the Treatment of BRAF-driven Cancers. ANNUAL MEETING, American Association for Cancer Research, 2023.
- [2]. Rudolph J, et al. Contemporary design of small-molecule kinase modulators: orthosteric, allosteric and induced-proximity strategies. Nature reviews. Drug discovery. 2026 Aug;25(8):595-618.
- [3]. Kreger B T, et al. CFT1946 Is an Orally Available Brain‑Penetrant BRAFV600‑Mutant Degrader That Overcomes BRAF Inhibitor Resistance. Cancer Research, 2026, 86(2):438‑452.
