PROTAC B-Raf degrader 1
- CAS NO.：2364367-27-9
- Empirical Formula: C36H37N5O12S
- Molecular Weight: 763.77
- Update Date: 2024-07-02 08:55:04
What is PROTAC B-Raf degrader 1?
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].
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.
Properties of PROTAC B-Raf degrader 1
| 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) |
| pka | 10.68±0.40(Predicted) |
| form | Solid |
| color | Light yellow to yellow |
Safety information for PROTAC B-Raf degrader 1
Computed Descriptors for PROTAC B-Raf degrader 1
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