PROTAC B-Raf degrader 1
- CAS NO.：2364367-27-9
- Empirical Formula: C36H37N5O12S
- Molecular Weight: 763.77
- Update Date: 2025-04-17 18:22:24
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
New Products
2-Ethoxyphenol Methyl 2-methoxy-5-sulfamoylbenzoate 3,6-Dichloropyridazine Ethyl 2-chloro-2-(2-(4-methoxyphenyl)hydrazono)acetate 3,6-Dichloro-4-Isopropylpyridazine 2-[(2-Ethoxyphenoxy)methyl]oxirane 4-Morpholinoaniline 2-Chloromethyl-6-methyl-pyridine 1-Indanone tert-Butyl ((1R,2S,5S)-2-amino-5-(dimethylcarbamoyl)cyclohexyl)carbamate 2-Pyridinecarboxaldehdye 6-Methyl-2-pyridinemethanol 4-Bromo-2-fluoro-N-methylbenzamide 3-Azetidinecarboxylic acid N-(2-(4-((4-Fluorobenzyl)carbamoyl)-5-hydroxy-6-methoxypyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazole-2-carboxamide (R)-4-Boc-morpholine-3-carboxylic acid (Required high chiral purity NLT:99.5%) Tetrahydro-3-(2-methyl-2- nitropropyl)-2H-pyran-2-one 3-Bromo-2-fluorobenzonitrile Desoximetasone Boron Triiodide Nicotinic acid RAPAMYCIN Pentachlorobenzonitrile BudesonideRelated products of tetrahydrofuran
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