PROTAC Bcl2 degrader-1 CAS#: 2378801-85-3

PROTAC Bcl2 degrader-1 Basic information

Product Name:

PROTAC Bcl2 degrader-1

Synonyms:

PROTAC Bcl2 degrader-1
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]-
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
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

CAS:

2378801-85-3

MF:

C45H45BrN6O10S

MW:

941.84

Mol File:

2378801-85-3.mol

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PROTAC Bcl2 degrader-1 Chemical Properties

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 Usage And Synthesis

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-1Supplier

Bide Pharmatech Ltd.

Tel: 400-164-7117 13681763483
Email: product02@bidepharm.com

Fan De(Beijing) Biotechnology Co., Ltd.

Tel: 15911056312
Email: liming@bio-fount.com

Jilin Province Woda Biotechnology Co., Ltd.

Tel: 13504435624
Email: 1927928688@qq.com

TargetMol Chemicals Inc.

Tel: +1-781-999-5354; +17819995354
Email: marketing@targetmol.com

ChemeGen(Shanghai) Biotechnology Co.,Ltd.

Tel: 18818260767
Email: sales@chemegen.com

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