Carfilzomib

Carfilzomib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

In July 2012, the US FDA approved carfilzomib (also referred to as PR-171) for the treatment of patients with multiple myeloma (MM) who have received at least two prior therapies including bortezomib and an immunomodulatory agent and have demonstrated disease progression within 60 days of completion of the last therapy. Carfilzomib binds to and irreversibly inhibits the chymotrypsin-like protease activity of the constitutive proteosome (β5) and immunoproteosome (β5i) via its epoxyketone pharmacophore. Proteosome inhibition results in the accumulation of polyubiquitinated proteins and induction of apoptosis through activation of both the intrinsic and extrinsic caspase pathways. Carfilzomib inhibits chymotrypsin activity with an IC₅₀ of 6 nM and is less potent an inhibitor of trypsin and caspase (IC_50s of 3600 and 2400 nM, respectively). Cell cycle arrest and apoptosis are seen in a variety of hematologic and solid tumor cell lines (e.g.,MM, acutemyeloid leukemia (AML), pancreatic cancer, lung cancer) treated with carfilzomib.

Chemische Eigenschaften

White Solid

Verwenden

Carfilzomib is a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma.

Definition

ChEBI: Carfilzomib is a synthetic tetrapeptide consisting of morpholin-4-acetyl, L-2-amino-4-phenylbutanoyl, L-leucyl and L-phenylalanyl residues joined in sequence with the C-terminus connected to the amino group of (2<element S)-2-amino-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-1-one via an amide linkage. Used for the treatment of patients with multiple myeloma.

Clinical Use

Carfilzomib is an irreversible inhibitor of the chymotrypsin-like protease in the proteasome and was approved in the U.S. for the treatment of multiple myeloma. Carfilzomib was discovered by Proteolix which was later acquired by Onyx Therapeutics who completed the development of this drug. Carfilzomib is also undergoing clinical evaluation for additional oncology indications such as relapsed solid tumors, lymphoma, prolymphocytic leukemia, acute myeloid leukemia and acute lymphocytic leukemia.

Carfilzomib Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Carfilzomib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
Shaanxi Haibo Biotechnology Co., Ltd	+undefined18602966907	qinhe02@xaltbio.com	China	1000	58
Hangzhou Hyper Chemicals Limited	+86-0086-57187702781 +8613675893055	info@hyper-chem.com	China	198	58
Alpha Biopharmaceuticals Co., Ltd	+86-15542445688	sales@alabiochem.com	China	888	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21677	55
Chembon Pharmaceutical Co., Ltd.	+86-28-8425-2981		CHINA	724	55
Hangzhou FandaChem Co.,Ltd.	008657128800458; +8615858145714	fandachem@gmail.com	China	9338	55
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32760	60
Lianyungang happen teng technology co., LTD	15950718863	wang666xt@163.com	CHINA	295	58
career henan chemical co	+86-0371-55982848 +86-15093356674	sales@coreychem.com	China	29901	58
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	967	58

868540-17-4()Verwandte Suche:

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• CarfilzoMib salt
• CarfilzoMib/PR 171
• PR 171
• PR-171 (CarfilzoMib)
• (alphaS)-alpha-[(4-Morpholinylacetyl)amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-L-phenylalaninamide
• Carfilzomib
• CarfilzoMib, Free Base, >99%
• (S)-4-Methyl-N-((S)-1-((S)-4-Methyl-1-((R)-2- Methyloxiran-2-yl)-1 -oxopentan-2-ylaMino)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-MorpholinoacetaMido)-4-phenylbutanaMido)pentanaMide
• L-Phenylalaninamide, (αS)-α-[[2-(4-morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-
• (alphaS)-alpha-[(4-Morpholinylacetyl)amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-L-phenylalaninamide Carfilzomib(PR171)
• Carfilzomib (alphaS)-alpha-[(4-Morpholinylacetyl)amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-L-phenylalaninamide
• Carfilzomib, >=99%
• (αS)-α-[[2-(4-Morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-L-phenylalaninamide
• (S)-4-Methyl-N-((S)-1-(((S)-4-methyl-1-((R)-2-methyloxiran-2-yl)-1-oxopentan-2-yl)amino)-1-oxo
• N-{(2S)-2-[(Morpholin-4-ylacetyl)aMino]-4-phenylbutanoyl}-L-leucyl-N-{(2S)-4-Methyl-1-[(2R)-2-Methyloxiran-2-yl]-1-oxopentan-2-yl}-L-phenylalaninaMide
• Carfilzomib API and intermediates
• Carfilzomib, 99%, irreversible proteasome inhibitor
• PR171;PR 171
• CS-603
• Carfilzomib API
• Carfilzomib (2R,4S)-Diol (7R)-Isomer
• Carfilzomib (2S,4S)-Diol (7R)-Isomer
• Carfilzomib (2S,4R)-Diol (7R)-Isomer
• Carfilzomib (2R,4R)-Diol (7R)-Isomer
• (S)-4-Methyl-N-[(S)-1-[[(S)-4-methyl-1-[(R)-2-methyloxiran-2-yl]-1-oxo-2-pentyl]amino]-1-oxo-3-phenyl-2-propyl]-2-[(S)-2-(2-morpholinoacetamido)-4-phenylbutanamido]pentanamide
• 7(R)-epi Carfilzomib (2R,4S)-diolQ: What is 7(R)-epi Carfilzomib (2R,4S)-diol Q: What is the CAS Number of 7(R)-epi Carfilzomib (2R,4S)-diol
• 7(R)-epi Carfilzomib (2S,4R)-diolQ: What is 7(R)-epi Carfilzomib (2S,4R)-diol Q: What is the CAS Number of 7(R)-epi Carfilzomib (2S,4R)-diol
• L-Phenylalaninamide, (αS)-α-[[2-(4-morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]- (Carfilzomib impurity)
• (αS)-α-[[2-(4-Morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-L-phenylalaninamide
• Carfilzomib（For R & D only）
• Carfezomil
• 868540-17-4
• 86854-17-4
• C40H57N5O7
• Inhibitors
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• API
• Inhibitor
• Pharmaceutical
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