PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity.
IC50&Target
B-Raf
体外研究
The IC50 values of PROTAC B-Raf degrader 1 (compound 2) towards MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells are 2.7 μM, 21.21 μM, 18.70 μM, 41.11μM and 22.68 μM, respectively.
PROTAC B-Raf degrader 1 (5 or 10 μM) can accelerate the degradation of B-Raf by recruiting ubiquitin-proteasome system, and further affects the expression of Mcl-1, a downstream protein of B-Raf.
MCF-7 cells achieve an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation of PROTAC B-Raf degrader 1 with the concentration of 20 μM.
PROTAC B-Raf degrader 1 arrests cell cycle at the G2/M phase.
Cell Cytotoxicity Assay
Cell Line:
Human MCF-7 breast cancer cell line, MDA-MB-231 breast cancer cells, human HepG2 hepatoma cells, human normal LO2 liver cells, B16 cells.
Concentration:
0-200 μM.
Incubation Time:
72 hours.
Result:
The IC50 values are 2.7 μM, 21.21 μM, 18.70 μM, 41.11μM and 22.68 μM in MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells, respectively.
Western Blot Analysis
Cell Line:
Human MCF-7 breast cancer cell line.
Concentration:
5 or 10 μM.
Incubation Time:
24 hours.
Result:
Effectively induced the degradation of B-Raf and impacted the expression of Mcl-1.
Apoptosis Analysis
Cell Line:
Human MCF-7 breast cancer cell line.
Concentration:
2.7-20 μM.
Incubation Time:
24 hours.
Result:
Achieved an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation with the concentration of 20 μM.
Cell Cycle Analysis
Cell Line:
Human MCF-7 breast cancer cell line.
Concentration:
20 μM.
Incubation Time:
24 hours.
Result:
1.94% cells were arrested at G1 phase, 8.20% at S phase, and 89.86% at G2/M phase.
分子量
763.77
CAS号
2364367-27-9
运输条件
Room temperature in continental US; may vary elsewhere.