| Company Name: |
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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| Tel: |
18818260767 |
| Email: |
sales@chemegen.com |
| Products Intro: |
Product Name:PROTAC B-Raf degrader 1
CAS:2364367-27-9
Purity:98% Package:10 mg;50 mg;100 mg;500 mg;1 g;5 g;10 g
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| Company Name: |
Guangzhou Younan Technology Co., Ltd
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| Tel: |
020-82000279 18988941452 |
| Email: |
YN_research@163.com |
| Products Intro: |
Product Name:PROTAC B-Raf degrader 1
CAS:2364367-27-9
Purity:0.98 Package:5mg;10mg;25mg;50mg;100mg
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| | PROTAC B-Raf degrader 1 Basic information |
| Product 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 | | CAS: | 2364367-27-9 | | MF: | C36H37N5O12S | | MW: | 763.77 | | EINECS: | | | Product Categories: | | | Mol File: | 2364367-27-9.mol |  |
| | PROTAC B-Raf degrader 1 Chemical Properties |
| 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 |
| | PROTAC B-Raf degrader 1 Usage And Synthesis |
| Uses | 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]. | | 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]. | | IC 50 | B-Raf | | 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 |
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