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Carfilzomib

CAS No.: 868540-17-4

Chemical Name:: Carfilzomib

Synonyms: PR 171;CS-603;Carfezomil;Carfilzomib;PR171;PR 171;Carfilzomib API;CarfilzoMib salt;CarfilzoMib/PR 171;Carfilzomib, >=99%;PR-171 (CarfilzoMib)

CBNumber:: CB12520831

Molecular Formula:: C40H57N5O7

Molecular Weight:: 719.92

MOL File:: 868540-17-4.mol

Modify Date:: 2024/5/9 14:42:29

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Carfilzomib Properties

Melting point	204 - 208°C
Boiling point	975.6±65.0 °C(Predicted)
Density	1.161
Flash point	543.8℃
storage temp.	-20°
solubility	Soluble in DMSO (up to 80 mg/ml) or in Ethanol (up to 25 mg/ml).
form	solid
pka	13.17±0.46(Predicted)
color	White
Stability	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 week.
CAS DataBase Reference	868540-17-4

SAFETY

Risk and Safety Statements

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302-H315-H319-H335
Precautionary statements	P261-P305+P351+P338
HS Code	29337900

Carfilzomib Chemical Properties,Uses,Production

Description

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.

Chemical Properties

White Solid

Uses

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 Preparation Products And Raw materials

Raw materials

Preparation Products

Carfilzomib Suppliers

Global( 351)Suppliers

Supplier	Tel	Country	ProdList	Advantage	Inquiry
AVD pharmaceuticals Pvt Ltd	+919860835260	Pune, India	102	58	Inquiry
Dr. Reddy's Laboratories Ltd	+91-4049002900 +91-4049002900	Hyderabad, India	165	58	Inquiry
J S LABS	+91-7330612784 +91-7330612784	Tamil Nadu, India	160	58	Inquiry
CHEMAZON LABORATORIES	+91 9848551964	Hyderabad, India	1320	58	Inquiry
Avra Laboratories Pvt Ltd	+91-8008572391 +91-8008572391	Hyderabad, India	43	58	Inquiry
Basil Drugs AND Pharmaceuticals Pvt Ltd	+91-2249700250 +91-9619320820	Mumbai, India	108	58	Inquiry
Sakar Healthcare	+91-8976292690 +91-9967572302	Gujarat, India	47	58	Inquiry
Biophore India Pharmaceuticals Pvt Ltd	+91-9100031592 +91-9030907714	Telangana, India	134	58	Inquiry
Beta Drugs	+91-9316590666 +91-7015991921	Haryana, India	34	58	Inquiry
Mylan Laboratories Ltd	+91-4023550543 +91-4030866666	Telangana, India	150	58	Inquiry

Supplier	Advantage
AVD pharmaceuticals Pvt Ltd	58
Dr. Reddy's Laboratories Ltd	58
J S LABS	58
CHEMAZON LABORATORIES	58
Avra Laboratories Pvt Ltd	58
Basil Drugs AND Pharmaceuticals Pvt Ltd	58
Sakar Healthcare	58
Biophore India Pharmaceuticals Pvt Ltd	58
Beta Drugs	58
Mylan Laboratories Ltd	58

Carfilzomib Spectrum

Carfilzomib(868540-17-4)¹HNMR

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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 peptides API Inhibitor Pharmaceutical 868540-17-4 Coronavirus