Carfilzomib (marketed under the trade name Kyprolis, developed by Onyx Pharmaceuticals) is an anti-cancer drug acting as a selective proteasome inhibitor. Chemically, it is a tetrapeptide epoxyketone and an analog of epoxomicin.
Carfilzomib is derived from epoxomicin, a natural product that was shown by the laboratory of Craig Crews at Yale University to inhibit the proteasome. The Crews laboratory subsequently invented a more specific derivative of epoxomicin named YU101, which was licensed to Proteolix, Inc. Scientists at Proteolix invented a new, distinct compound that had potential use as a drug in humans, known as carfilzomib. Proteolix advanced carfilzomib to multiple Phase 1 and 2 clinical trials, including a pivotal phase 2 clinical trial designed to seek accelerated approval. Clinical trials for carfilzomib continue under Onyx Pharmaceuticals, which acquired Proteolix in 2009.
Carfilzomib covalently irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S proteasome, an enzyme that degrades unwanted cellular proteins. Carfilzomib displays minimal interactions with non-proteasomal targets, thereby improving safety profiles over bortezomib. Inhibition of proteasome-mediated proteolysis results in a build-up of polyubiquitinated proteins, which may cause cell cycle arrest, apoptosis, and inhibition of tumor growth.
Huateng Pharma developed several kinds of intermediates for Carfilzomib with high quality & fast shipping. We are able to provide the services of Anti-Cancer intermediates’ process development and scale-up production with capacities varying from gram to kilograms and multi tons.
Today I want to introduce two kinds of intermediates for Carfilzomib from Huateng Pharma.
Product name: 1-Pentanone,2-amino-4-methyl-1-[(2R)-2-methyl-2-oxiranyl]-,(2S)-,2,2,2-trifluoroacetate(1:1)
CAS NO.: 247068-85-5
Catalog ID: 98534
Molecular formula: C9H17NO2.C2Hf3O2
Molecular weight: 285.26
Product name: (S)-methyl 2-((S)-2-tert.butoxycarbonyIamino-4-phenylbutanamido-4-methylpentanamido)-3-phenylpropanoate
CAS NO.: 868539-96-2
Catalog ID: 99702
Molecular formula: C31H43N3O6
Molecular weight: 553.696