PROTAC B-Raf degrader 1
- Product Name
- PROTAC B-Raf degrader 1
- CAS No.
- 2364367-27-9
- Chemical Name
- PROTAC B-Raf degrader 1
- Synonyms
- PROTAC B-Raf degrader 1;N-({[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]carbamoyl}methyl)-2-[(2-methoxy-5-{[(1E)-2-(2,4,6-trimethoxyphenyl)ethenesulfonyl]methyl}phenyl)amino]acetamide
- CBNumber
- CB25848913
- Molecular Formula
- C36H37N5O12S
- Formula Weight
- 763.77
- MOL File
- Mol file
PROTAC B-Raf degrader 1 Property
- 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
N-Bromosuccinimide Price
- Product number
- CS-0090791
- Product name
- PROTACB-Rafdegrader1
- Purity
- 99.18%
- Packaging
- 5mg
- Price
- $580
- Updated
- 2021/12/16
- Product number
- CS-0090791
- Product name
- PROTACB-Rafdegrader1
- Purity
- 99.18%
- Packaging
- 10mg
- Price
- $980
- Updated
- 2021/12/16
PROTAC B-Raf degrader 1 Chemical Properties,Usage,Production
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.
PROTAC B-Raf degrader 1 Preparation Products And Raw materials
Raw materials
Preparation Products
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