Carfilzomib

SKU: orb1307429

Description

Carfilzomib

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 868540-17-4
• MW: 719.91
• Purity: 99.84%
• 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: Autophagy,Apoptosis,Proteasome
• Solubility: DMSO:242 mg/mL (336.15 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5.5 mg/mL (7.64 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

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 prolonge the survival time o 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 decrease the cell viability of RPMI 8226 and ANBL-6 cells, with IC50 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 an the extent of apoptosis was time dependent.
• Cell Research:
  WST-1 is used to determin 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 interpolat the median inhibitory concentration IC50 using XLfit 4 software the degree of resistance (DOR) is calculated usin 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 o the mitochondrial membrane potential-dependent color shift from 525 to 590 nM is carried out on a FacScan, an the data are analyzed with CellQuest software.(Only for Reference)

Storage & Handling

• Storage: keep away from direct sunlight | Powder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Carfilzomib, Apoptosis, Autophagy, inhibit, Inhibitor, Proteasome, PR 171, PR171, PR-171

Compound Identifiers

PubChem CID

11556711