Tagarafdeg

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[1][2].

Product Specifications

CAS Number

[2882165-79-7]

Product Name Alternative

CFT1946

UNSPSC

12352005

Target

PROTACs; Raf

Type

Reference compound

Related Pathways

MAPK/ERK Pathway; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/cft1946.html

Purity

99.41

Solubility

DMSO : 100 mg/mL (ultrasonic)

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

Molecular Formula

C45H49F2N11O9S

Molecular Weight

958.00

References & Citations

[1]Sowa M E, et al. Preclinical evaluation of CFT1946 as a selective degrader of mutant BRAF for the treatment of BRAF driven cancers[J]. Cancer Research, 2022, 82 (12_Supplement) : 2158-2158.|[2]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.