ChemicalBook > CAS DataBase List > PROTAC Bcl2 degrader-1
PROTAC Bcl2 degrader-1
- Product Name
- PROTAC Bcl2 degrader-1
- CAS No.
- 2378801-85-3
- Chemical Name
- PROTAC Bcl2 degrader-1
- Synonyms
- PROTAC Bcl2 degrader-1;N1-(2-(6-((4-Bromophenyl)thio)-1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)ethyl)-N6-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethyl)adipamide;Hexanediamide, N1-[2-[6-[(4-bromophenyl)thio]-1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl]ethyl]-N6-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethyl]-;N'-(2-{8-[(4-bromophenyl)sulfanyl]-2,4-dioxo-3-azatricyclo[7.3.1.0?,13]trideca-1(13),5,7,9,11-pentaen-3-yl}ethyl)-N-{2-[2-(2-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}ethoxy)ethoxy]ethyl}hexanediamide
- CBNumber
- CB85821213
- Molecular Formula
- C45H45BrN6O10S
- Formula Weight
- 941.84
- MOL File
- 2378801-85-3.mol
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PROTAC Bcl2 degrader-1 Property
- Boiling point:
- 1158.2±65.0 °C(Predicted)
- Density
- 1.54±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 25 mg/mL (26.54 mM)
- pka
- 10.74±0.40(Predicted)
- form
- Solid
- color
- Light yellow to yellow
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PROTAC Bcl2 degrader-1 Chemical Properties,Usage,Production
Uses
PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1[1] (Blue: CRBN ligand, Black: linker;Pink: Mcl-1/Bcl-2 inhibitor, Nap-1).
IC 50
Bcl-2: 3 μM (DC50); Bcl-2: 4.94 μM (IC50); Mcl-1: 11.81 μM (IC50)
References
[1] Wang Z, et al. Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands. J Med Chem. 2019 Aug 21. DOI:10.1021/acs.jmedchem.9b00919
PROTAC Bcl2 degrader-1 Preparation Products And Raw materials
Raw materials
Preparation Products
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