Solubility: Soluble in DMSO (up to 80 mg/ml) or ethanol (up to 25 mg/ml)
pKa: 13.17±0.46 (Predicted)
Polarizability: 78.3±0.5 10^-24 cm³
Refractive Index: 1.551
Vapor Pressure: 0.0±0.3 mmHg (at 25°C)
Storage Conditions: Typically stored at -20°C
III. Chemical Properties
Chemical Structure: Carfilzomib is an epoxyketone proteasome inhibitor with a tetrapeptidyl epoxide skeleton that irreversibly binds to the N-terminal threonine active site of the 20S proteasome and the proteolytic core particle of the 26S proteasome.
Mechanism of Action: As an irreversible proteasome inhibitor, Carfilzomib selectively binds to both constitutive and immunoproteasomes, inhibiting proteolysis, leading to the accumulation of polyubiquitinated proteins, which in turn triggers cell cycle arrest, induction of apoptosis, and inhibition of tumor growth.
IV. Uses and Benefits
Primary Use: Carfilzomib is primarily used for the treatment of relapsed or refractory multiple myeloma (MM). Multiple myeloma is a malignant plasma cell disease that occurs in B lymphocytes and is the second most common hematological malignancy globally.
Clinical Effects: In clinical trials, Carfilzomib has demonstrated significant efficacy in improving objective response rates and progression-free survival for patients. It is typically administered intravenously, with specific doses and treatment schedules determined based on the patient's condition and body weight.
