CFT1946 free base · Synonyms: CFT-1946 · CFT 1946
CFT1946 is an orally active and selective target ligand.
For research use only. Not for human or veterinary use.
Purity >98%
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CFT1946 structure
CAS No.: 2882165-79-7
Pack sizes & pricing
Description
CFT1946 is an orally active and selective target ligand for BRAF kinase. CFT1946 is a degrader of mutant BRAFV600E, G469A, G466V and p61-BRAFV600E. CFT1946 can be used in tumor research.
Biological activity
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 Tagarafdeg (CFT1946) (0.3-10 mg/kg; PO; BID; 20 days) induces tumor regression in the BRAFV600E A375 xenograft mouse model with 10 mg/kg
Identifiers
- 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 - InChIKey
-
OCDRMYDQTIPVOI-HHHXNRCGSA-N
Specifications
- MW (average)
- 958.0010
- Formula
- C45H49F2N11O9S
- CAS No.
- 2882165-79-7
- Physical state
- Solid
- Color
- Off-white to light yellow
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃ 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO
- In vitro
- DMSO : 100 mg/mL
Documents
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.
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