26.05.2020 08:29:38 -

( - 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 irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S catalytic core subunit of the proteasome. Proteasome is part of the cellular machinery and has many functions within the cell, such as it helps to control the level of many of the proteins that help to regulate cell division and cell survival. By interfering with its function this can lead to apoptosis (cell suicide). In the laboratory, it has been shown that cancer cells are more susceptible to the effects of proteasome inhibitors than normal cells are.

Carfilzomib exerts its anti-myeloma activity through a variety of actions, including induction of unfolded protein stress response, down-regulation of NF-κB prosurvival activity, modification of bone turnover and the bone marrow microenvironment, leading to increased bone strength compromised microenvironmental support for myeloma cells, and induction of immunogenic myeloma cell death through increased natural kill cell-mediated MM-cell lysis and enhanced antigen presentation. Carfilzomib has a different structure (tetrapeptide epoxyketone) from the first generation PI bortezomib (dipeptide boronate). Preclinical studies have shown that carfilzomib can overcome the resistance of bortezomib without reducing neurite length or inhibiting non-proteasomal targets such as HtrA2 / Omi, which was observed in bortezomib. Compared to bortezomib, carfilzomib causes deeper, longer-lasting proteasome inhibition.

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
Purity: 98%
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
Purity: 98%
Molecular formula: C31H43N3O6
Molecular weight: 553.696

Hunan Huateng Pharmaceutical Co., Ltd. , founded in August 2013​, is a high-tech enterprise dedicated to the research and development and production of high-end biomedical chemical products, as well as the development of precision-targeted anti-tumor drugs. The company develops and produces thousands of products, including monodisperse and polydisperse PEG derivatives, high-end biochemical reagents, pharmaceutical intermediates, APIs, preparations and targeted anti-tumor drugs.

Hunan Huateng Pharmaceutical Co., Ltd. has a research and development production base of 5,000 square meters in Changsha High-tech Zone, and another 37,000 square meters of APIs and preparation manufacturing plant under construction. After the completion of the production base, the company's annual production capacity of biomedical products will reach more than 5 billion yuan. The company's R&D center is equipped with high-end analytical instruments and high-end automatic reaction equipment, such as 400M NMR, Agilent LCMS, HPLC, GC, IR, GPC, automatic polarimeter, constant moisture titrator, low temperature reactor, high pressure hydrogenation reaction. We have our own R&D and logistics centers in China, the United States, Europe and many other countries. And we have set up an excellent and efficient R&D production and sales professional team to provide one-stop service for professional, personalized and technical support to all customers worldwide.

Press Information:
Hunan Huateng Pharmaceutical Co. Ltd

Lugu Business Plaza E1, Yuelu District, Changsha City, Hunan Province, P.R. China.

Contact Person:
Sonia Lee

Phone: 073189916275
eMail: eMail



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