For research use only. Not for therapeutic Use.
SJF-0628 (compound 512) is a PROTAC RAF degrader. SJF-0628 induces targeted degradation of BRAF mutants (DC50: 5.4 nM, 4.64 nM, 15.5 nM, 2.11 nM, 63.9 nM for BRAF V600E, V600K, G464V, G469A, K601E respectively). SJF-0628 has anti-tumor activity. SJF-0628 can be used for research of disorders that result from aggregation or accumulation of RAF, or the constitutive activation of RAF[1].
Catalog Number | I036330 |
CAS Number | 2413035-41-1 |
Synonyms | (2S,4R)-1-[(2S)-2-[[2-[4-[4-[3-[2,6-difluoro-3-(propylsulfonylamino)benzoyl]-1H-pyrrolo[2,3-b]pyridin-5-yl]phenyl]piperazin-1-yl]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide |
Molecular Formula | C51H57F2N9O7S2 |
Purity | ≥95% |
InChI | InChI=1S/C51H57F2N9O7S2/c1-6-21-71(68,69)59-40-16-15-39(52)43(44(40)53)45(65)38-26-55-48-37(38)22-34(25-54-48)32-11-13-35(14-12-32)61-19-17-60(18-20-61)28-42(64)58-47(51(3,4)5)50(67)62-27-36(63)23-41(62)49(66)56-24-31-7-9-33(10-8-31)46-30(2)57-29-70-46/h7-16,22,25-26,29,36,41,47,59,63H,6,17-21,23-24,27-28H2,1-5H3,(H,54,55)(H,56,66)(H,58,64)/t36-,41+,47-/m1/s1 |
InChIKey | MBCAVOCJJAQHHT-FGUOTCRGSA-N |
SMILES | CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=C2C=C(C=N3)C4=CC=C(C=C4)N5CCN(CC5)CC(=O)NC(C(=O)N6CC(CC6C(=O)NCC7=CC=C(C=C7)C8=C(N=CS8)C)O)C(C)(C)C)F |
Reference | [1]. Andrew P. Crew, et al. Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides. Patent. US 20200129627 A1. [2]. 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. |