Free shipping on all orders over $ 500

E3 ligase Ligand 1

Cat. No. M9826
E3 ligase Ligand 1 Structure
Synonym:

VHL ligand 2 hydrochloride; (S,R,S)-AHPC-Me hydrochloride

Size Price Availability Quantity
100mg USD 90  USD90 In stock
500mg USD 300  USD300 In stock
1g USD 480  USD480 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

E3 ligase Ligand 1 (VHL ligand 2 hydrochloride; (S,R,S)-AHPC-Me hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride 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 DC50 <1 nM.

Chemical Information
Molecular Weight 481.05
Formula C23H33ClN4O3S
CAS Number 1948273-03-7
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kanak Raina, et al. Proc Natl Acad Sci U S A. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

Related Ligand for E3 Ligase Products
2,6-bis(benzyloxy)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine

2,6-bis(benzyloxy)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine

2,6-Bis(benzyloxy)pyridine-3-boronic acid

2,6-Bis(benzyloxy)pyridine-3-boronic acid

2,6-Bis(benzyloxy)-3-bromopyridine

2,6-Bis(benzyloxy)-3-bromopyridine

2,6-bis(benzyloxy)pyridin-3-amine

2,6-bis(benzyloxy)pyridin-3-amine

3-[2,5-Difluoro-4-(4-piperidinyl)phenyl]-2,6-piperidinedione

3-[2,5-Difluoro-4-(4-piperidinyl)phenyl]-2,6-piperidinedione

  Catalog
Abmole Inhibitor Catalog




Keywords: E3 ligase Ligand 1, VHL ligand 2 hydrochloride; (S,R,S)-AHPC-Me hydrochloride supplier, Ligand for E3 Ligase, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.