[CAS NO. 2504950-56-3] (S,R,S)-AHPC-Medihydrochloride
PRODUCTS SPECIFICATIONS [2504950-56-3]
DESCRIPTION [2504950-56-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 517.51 |
| Molecular Formula | C23H34Cl2N4O3S |
| SMILES | N[C@@H](C(C)(C)C)C(N1[C@H](C(N[C@@H](C)C2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O.Cl.Cl |
Summary
(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein [1] . (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC 50 <1 nM [2] .
IC50 & Target
|
VHL |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 100 mg/mL ( 193.23 mM ; Need ultrasonic)
DMSO : 50 mg/mL ( 96.62 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9323 mL | 9.6616 mL | 19.3233 mL |
| 5 mM | 0.3865 mL | 1.9323 mL | 3.8647 mL |
| 10 mM | 0.1932 mL | 0.9662 mL | 1.9323 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (193.23 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5 mg/mL (9.66 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 5 mg/mL (9.66 mM); Clear solution
