Carfilzomib CAS 868540-17-4 API
Carfilzomib is a sterile, white to off-white lyophilized powder and is available as a single-use vial. Carfilzomib is a modified tetrapeptidyl epoxide, isolated as the crystalline free base.
Description
Carfilzomib is a sterile, white to off-white lyophilized powder and is available as a single-use vial. Carfilzomib is a modified tetrapeptidyl epoxide, isolated as the crystalline free base.
The chemical name for carfilzomib is (2S)-N-((S)-1-((S)-4-methyl-1-((R)-2-methyloxiran[1]2-yl)-1-oxopentan-2-ylcarbamoyl)-2-phenylethyl)-2-((S)-2-(2-morpholinoacetamido)4-phenylbutanamido)-4-methylpentanamide.
Carfilzomib is a crystalline substance with a molecular weight of 719.9. The molecular
formula is C40H57N5O7. Carfilzomib is practically insoluble in water, and very slightly
soluble in acidic conditions.
Basic Information
|
Chemical Name |
Carfilzomib |
|
CAS NO. |
868540-17-4 |
|
Appearance |
White to off-white powder |
|
Molecular Formula |
C40H57N5O7 |
|
Molecular Weight |
719.9 |
|
Purity by Genohope |
99% |
|
Annual Capacity by Genohope |
50-100 kg/year |
|
Process by Genohope |
Fully Synthesis or Ecoli Fermentation |
|
Molecular Structure |
|
Brief Introduction
Carfilzomib, developed by Onyx Pharmaceuticals and sold under the brand name Kyprolis, is an anti-cancer medication acting as a selective proteasome inhibitor.
Chemically, it is a tetrapeptide epoxyketone and an analog of epoxomicin.
Carfilzomib was approved by The US Food and Drug Administration (FDA) in July 2012.
Indication and Usage
Carfilzomib is indicated for the treatment of patients with multiple myeloma who have received at least two prior therapies including bortezomib and an immunomodulatory agent and have demonstrated disease progression on or within 60 days of completion of the last therapy. Approval is based on response rate. Clinical benefit, such as improvement in survival or symptoms, has not been verified.
Mechanism of Action
Carfilzomib is a tetrapeptide epoxyketone proteasome inhibitor that irreversibly binds to the N-terminal threonine-containing active sites of the 20S proteasome, the proteolytic core particle within the 26S proteasome. Carfilzomib had antiproliferative and proapoptotic activities in vitro in solid and hematologic tumor cells. In animals, carfilzomib inhibited proteasome activity in blood and tissue and delayed tumor growth in models of multiple myeloma, hematologic, and solid tumors.
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