| Identification | Back Directory | [Name]
PROTAC B-Raf degrader 1 | [CAS]
2364367-27-9 | [Synonyms]
PROTAC B-Raf degrader 1 | [Molecular Formula]
C36H37N5O12S | [Molecular Weight]
763.77 |
| Chemical Properties | Back Directory | [Boiling point ]
1136.9±65.0 °C(Predicted) | [density ]
1.451±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C, stored under nitrogen | [solubility ]
DMSO : 25 mg/mL (32.73 mM; Need ultrasonic) | [form ]
Solid | [pka]
10.68±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Biological Activity]
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[1].
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[1].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[1].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[1].PROTAC B-Raf degrader 1 arrests cell cycle at the G2/M phase[1]. | [storage]
Store at -20°C, stored under nitrogen | [References]
[1]. Chen H, et al. Pomalidomide hybrids act as proteolysis targeting chimeras: Synthesis, anticancer activity and B-Raf degradation. Bioorg Chem. 2019 Mar 19;87:191-199. |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 13348960310 |
| Website: |
http://www.weikeqi-biotech.com/ |
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