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 H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
Protheragen-ING	+16313385890	info@protheragen-ing.com	United States	3868	58
Shaanxi Haibo Biotechnology Co., Ltd	+undefined18602966907	qinhe02@xaltbio.com	China	997	58
Hangzhou Hyper Chemicals Limited	+86-0086-57187702781 +8613675893055	info@hyper-chem.com	China	310	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21586	55
Chembon Pharmaceutical Co., Ltd.	+86-28-8425-2981		CHINA	722	55
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	33024	60
Lianyungang happen teng technology co., LTD	15950718863	wang666xt@163.com	CHINA	295	58
career henan chemical co	+86-0371-86658258 +8613203830695	sales@coreychem.com	China	29812	58
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	965	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19936	58

868540-17-4()Verwandte Suche:

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• CarfilzoMib salt
• CarfilzoMib/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)
• Carfilzomib（For R & D only）
• Carfezomil
• Caffezomib
• Carfilzomib, proteasome inhibitor
• Kafezomi
• Carfilzomib Impurity 88
• Carfilzomib Impurity 89
• Carfilzomib Impurity 90
• Carfilzomib Impurity 94 Chloride
• Carfilzomib Impurity 108
• Carfilzomib Impurity 105
• Carfilzomib Impurity 100
• Carfilzomib Impurity 87
• Carfilzomib Impurity 93
• Carfilzomib Impurity 104
• Carfilzomib Impurity 106
• Carfilzomib Impurity 107
• Carfilzomib Impurity 59 Monomer
• Carfilzomib Impurity 93 Chloride
• Carfilzomib Impurity 96
• Carfilzomib Impurity 99
• Carfilzomib Impurity 102
• Carfilzomib Impurity 86
• Carfilzomib Impurity 94
• Carfilzomib Impurity 109
• PR 171
• 868540-17-4
• 86854-17-4
• C40H57N5O7
• Inhibitors
• peptides