Carfilzomib

SKU: orb1307429

Description

Carfilzomib

Research Area

Cell Biology, Immunology & Inflammation, Protein Biochemistry

Key Properties

• CAS Number: 868540-17-4
• MW: 719.93
• Purity: >98%
• Formula: C₄₀H₅₇N₅O₇
• SMILES: CC(C)C[C@H](NC(=O)[C@H](CCc1ccccc1)NC(=O)CN1CCOCC1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)[C@@]1(C)CO1
• Target: Proteasome
• Solubility: Soluble in DMSO (up to 80 mg/ml) or in Ethanol (up to 25 mg/ml).

Bioactivity

• Target IC50:
  Proteasome:5 nM
• In Vivo:
  METHODS: To assay anti-tumor activity in vivo, Carfilzomib (5 mg/kg, 10% captisol) was injected intravenously twice weekly for five weeks into SCID mice bearing a mantle cell lymphoma (MCL) Mino. RESULTS: Carfilzomib virtually eliminated tumor growth and significantly prolonged the survival time of the tumor-bearing mice. METHODS: To detect anti-tumor activity in vivo, Carfilzomib (6 mg/kg, 10% captisol) was administered intraperitoneally three times a week for three weeks to a mouse model of metastatic amorphous thyroid tumor (ATC). RESULTS: Carfilzomib treatment of mice with established extensive metastatic disease significantly improved their survival without significant toxicity.
• In Vitro:
  METHODS: Myeloma cell lines RPMI 8226 and ANBL-6 were treated with Carfilzomib (0-25 nM) for 24 h, and cell viability was measured using WST-1 assay. RESULTS: Carfilzomib treatment dose-dependently decreased the cell viability of RPMI 8226 and ANBL-6 cells, with IC50s of less than 5 nM. METHODS: B-cell lymphoma cell lines Raji, Raji-2R and Raji-4RH were treated with Carfilzomib (1-10 nM) for 24-72 h. Apoptosis was analyzed using Flow Cytometry. RESULTS: Carfilzomib induced apoptosis in B-cell lymphoma cell lines and the extent of apoptosis was time dependent.
• Cell Research:
  WST-1 is used to determine the effects of proteasome inhibitor Carfilzomib on cell proliferation. The inhibition of proliferation is calculated in relation to parallel control cells that receives vehicle alone. A linear spline function is used to interpolate the median inhibitory concentration (IC50) using XLfit 4 software. The degree of resistance (DOR) is calculated using the formula: DOR = IC50(resistant cells)/IC50(sensitive cells). ANBL-6 cells pulsed with 100 nM carfilzomib are washed and suspended in PBS containing 5 μg/mL of JC-1, which exhibits potential-dependent accumulation in mitochondria. Analysis of the mitochondrial membrane potential-dependent color shift from 525 to 590 nm is carried out on a FacScan, and the data are analyzed with CellQuest software.(Only for Reference)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PR-171

Compound Identifiers

PubChem CID

11556711