Trade names Kyprolis
Other names PX-171-007
CAS Number 868540-17-4
Formula C40H57N5O7
Molar mass 719.924 g·mol−1
卡非佐米/Carfilzomib,是一种选择性蛋白酶体抑制剂。在化学上,它是一种四肽环氧酮(tetrapeptide epoxyketone)和环氧霉素(epoxomicin)的类似物。此成分是由Onyx Pharmaceuticals研发而出的。
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.
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