2413035-41-1
Chemical Structure
SJF-0628
- CAS No.: 2413035-41-1
- Formula:C51H57F2N9O7S2
- Molecular Weight:1010.18
IUPAC Name: (2S,4R)-1-((S)-2-(2-(4-(4-(3-(2,6-difluoro-3-(propylsulfonamido)benzoyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
InChIKey: MBCAVOCJJAQHHT-FGUOTCRGSA-N
SMILES: O=C([C@H]1N(C([C@@H](NC(CN2CCN(C3=CC=C(C4=CN=C(NC=C5C(C6=C(F)C=CC(NS(=O)(CCC)=O)=C6F)=O)C5=C4)C=C3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7
Biological Activity: SJF-0628 is a PROTAC degrader of BRAF mutants, with a DC50 of 6.8 nM against BRAFV600E. SJF-0628 induces the ubiquitination and degradation of BRAF mutants in various cancer cell lines. SJF-0628 reduces pMEK and pErk levels. SJF-0628 exhibits antitumor activity. SJF-0628 can be used in research on colorectal cancer, melanoma, lung cancer, and triple-negative breast cancer[1][2][3][4].
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SJF-0628 | 99.90% | SJF-0628 is a PROTAC degrader of BRAF mutants, with a DC50 of 6.8 nM against BRAFV600E. SJF-0628 induces the ubiquitination and degradation of BRAF mutants in various cancer cell lines. SJF-0628 reduces pMEK and pErk levels. SJF-0628 exhibits antitumor activity. SJF-0628 can be used in research on colorectal cancer, melanoma, lung cancer, and triple-negative breast cancer. | ||||||||||||||||||||
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References
- [1]. Chapdelaine AG, et al. The Targeted Degradation of BRAF V600E Reveals the Mechanisms of Resistance to BRAF-Targeted Treatments in Colorectal Cancer Cells. Cancers (Basel). 2023 Dec 12;15(24):5805. [Content Brief]
- [2]. Alabi S, et al. Mutant-selective degradation by BRAF-targeting PROTACs. Nat Commun. 2021 Feb 10;12(1):920. [Content Brief]
- [3]. He M, et al. Opportunities and Challenges of Small Molecule Induced Targeted Protein Degradation. Frontiers in cell and developmental biology. 2021;9:685106. [Content Brief]
- [4]. Han X, et al. PROTACs: A novel strategy for cancer drug discovery and development. MedComm. 2023 Jun;4(3):e290. [Content Brief]
