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.

 

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.

 

 

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

 

 

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.

 

 

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.

 

 

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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