Carfilzomib

Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.

Product Specifications

CAS Number

[868540-17-4]

Product Name Alternative

PR-171

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; Proteasome

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Metabolic Enzyme/Protease

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Carfilzomib.html

Purity

99.98

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

C[C@@]1(C([C@H](CC(C)C)NC([C@@H](NC([C@H](CC(C)C)NC([C@@H](NC(CN2CCOCC2)=O)CCC3=CC=CC=C3)=O)=O)CC4=CC=CC=C4)=O)=O)OC1

Molecular Formula

C40H57N5O7

Molecular Weight

719.91

Precautions

H302, H315, H319, H335

References & Citations

[1]Kawada T, Iwai K. In vivo and in vitro metabolism of dihydrocapsaicin, a pungent principle of hot pepper [Capsicum annuum], in rats[J]. Agricultural and Biological Chemistry (Japan), 1985, 49 (2) .|[2]Yang J, et al. Pharmacokinetics, pharmacodynamics, metabolism, distribution, and excretion of carfilzomib in rats. Drug Metab Dispos. 2011 Oct;39 (10) :1873-82.|[3]Efentakis P, et al. Molecular mechanisms of carfilzomib-induced cardiotoxicity in mice and the emerging cardioprotective role of metformin. Blood. 2019 Feb 14;133 (7) :710-723.|[4]Panagiotis Efentakis, et al. Carfilzomib-Induced Hypertension Is Mediated By Ion Channel Dysregulation in the Kidneys; The Potent Role of AMP-Activated Kinase α. Blood, Volume 136, Supplement 1, 2020, Pages 34-35, ISSN 0006-4971.