[CAS NO. 2378801-85-3] PROTACBcl2degrader-1
PRODUCTS SPECIFICATIONS [2378801-85-3]
DESCRIPTION [2378801-85-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 941.84 |
| Molecular Formula | C45H45BrN6O10S |
| SMILES | O=C(NCCOCCOCCNC1=CC=CC(C(N2C3CCC(NC3=O)=O)=O)=C1C2=O)CCCCC(NCCN4C(C5=C6C(C4=O)=CC=C(C6=CC=C5)SC7=CC=C(C=C7)Br)=O)=O |
Summary
PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 ( IC 50 , 4.94 μM; DC 50 , 3.0 μM) and Mcl-1 ( IC 50 , 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1 [1] .
IC50 & Target
|
Bcl-2 3 μM (DC 50 ) |
Bcl-2 4.94 μM (IC 50 ) |
Mcl-1 11.81 μM (IC 50 ) |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 25 mg/mL ( 26.54 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.0618 mL | 5.3088 mL | 10.6175 mL |
| 5 mM | 0.2124 mL | 1.0618 mL | 2.1235 mL |
| 10 mM | 0.1062 mL | 0.5309 mL | 1.0618 mL |
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