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Carfilzomib

description Mechanism Side effects Efficacy and Safety
Carfilzomib
Carfilzomib structure
CAS No.
868540-17-4
Chemical Name:
Carfilzomib
Synonyms
PR 171;CS-603;Kyprolis;Carfilzomib;PR171;PR 171;Carfilzomib API;CarfilzoMib salt;Carfilzomib, >=99%;CarfilzoMib/PR 171;PR-171 (CarfilzoMib)
CBNumber:
CB12520831
Molecular Formula:
C40H57N5O7
Formula Weight:
719.90988
MOL File:
868540-17-4.mol

Carfilzomib Properties

Boiling point:
975.6±65.0 °C(Predicted)
Density 
1.161
Flash point:
543.8℃
pka
13.17±0.46(Predicted)
CAS DataBase Reference
868540-17-4
FDA UNII
72X6E3J5AR
NCI Dictionary of Cancer Terms
carfilzomib; Kyprolis
SAFETY
  • Risk and Safety Statements
HS Code  29337900

Carfilzomib price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 17554 Carfilzomib ≥98% 868540-17-4 1mg $35 2020-06-24 Buy
Cayman Chemical 17554 Carfilzomib ≥98% 868540-17-4 5mg $158 2020-06-24 Buy
Cayman Chemical 17554 Carfilzomib ≥98% 868540-17-4 10mg $263 2020-06-24 Buy
Cayman Chemical 17554 Carfilzomib ≥98% 868540-17-4 50mg $569 2020-06-24 Buy

Carfilzomib Chemical Properties,Uses,Production

description

Carfilzomib is an irreversible proteasome inhibitor and antineoplastic agent.The mechanism of action of carfilzomib is as a Proteasome Inhibitor, Carfilzomib irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S catalytic core subunit of the proteasome, a protease complex responsible for degrading a large variety of cellular proteins. Inhibition of proteasome-mediated proteolysis results in an accumulation of polyubiquinated proteins, which may lead to cell cycle arrest, induction of apoptosis, and inhibition of tumor growth.
Carfilzomib is used in treatment of refractory multiple myeloma. Carfilzomib is associated with a low rate of serum enzyme elevations during treatment and has been implicated to rare instances of clinically apparent, acute liver injury some of which have been fatal.
Carfilzomib is a second-generation, irreversible, peptide epoxyketone class proteasome inhibitor that targets the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC50 = 5.2 nM) and the β5i subunit of the immunoproteasome 20Si (LMP7; IC50 = 14 nM) with minimal cross reactivity to other proteases. It can induce cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma, lymphoma, and various solid tumors (IC50s = 2.4-20 nM).

Mechanism

Carfilzomib is a tetrapeptide-based epoxy-proteasome inhibitor that irreversibly binds to the 20S proteasome containing the threonine N-terminal active site and the in vivo proteolysis core particle of 26S proteasome. In animal, carfilzomib has antiproliferative and apoptosis activity in vitro in solid and hematological granulocytes. In animals, carfilzomib inhibits proteasome activity in blood and tissue and delays tumor growth in multiple myeloma, hematological and solid tumor models.

Side effects

The most common adverse events observed in clinical trials (incidence ≥30%) were fatigue, anemia, nausea, thrombocytopenia, dyspnea, diarrhea and fever; the most common serious adverse events (overall incidence 45%) include pneumonia, acute renal failure, fever and congestive heart failure.

Efficacy and Safety

To assess the safety and efficacy of the drug, one study included 266 patients who had received at least two prior therapies, including bortezomib and thalidomide. It was assessed of the complete or partial disappearance of the tumor in the treated patient (overall response rate). The overall response rate was 23% and the median response time was 7.8 months.
Common adverse effects of carfilzomib were observed in more than 30% of the subjects include fatigue, low blood cell counts and platelet counts, dyspnea, diarrhea and fever. Severe adverse reactions include heart failure and dyspnea. Upon the occurrence of serious adverse reactions, the patient should be closely monitored and stop the drug treatment.
Information regarding the pharmacological effects, indications, mechanism of action, indications and side effects of Carfilzomib, a drug for treating multiple myeloma (MM), were compiled and edited by Xiao Nan of ChemicalBook.

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 (IC50s 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. The synthesis of carfilzomib is reported in the patent literature and a route to the intermediate epoxy ketone from a Boc-leucine-derived α,β-unsaturated ketone is also described.

Chemical Properties

White Solid

Originator

Proteolix Inc. (United States)

Uses

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

Definition

ChEBI: 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

brand name

Kyprolis

Carfilzomib Preparation Products And Raw materials

Raw materials

Preparation Products


Carfilzomib Suppliers

Global( 212)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Shenzhen Nexconn Pharmatechs Ltd
15013857715
admin@nexconn.com CHINA 3035 58
BOC Sciences
1-631-619-7922
1-631-614-7828 inquiry@bocsci.com United States 20039 58
Alpha Biopharmaceuticals Co., Ltd
0086-411-39042497
0086-411-39042693 sales@alphabiopharm.com China 921 58
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21821 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22626 55
Chembon Pharmaceutical Co., Ltd.
+86-28-8425-2981
+86-28-8425-2965 info@chembon.com CHINA 724 55
PI & PI BIOTECH INC.
18371201331
020-81716319 Sales@pipitech.com CHINA 3050 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24723 60
Lianyungang happen teng technology co., LTD
15950718863
wang666xt@163.com CHINA 296 58
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30045 58

View Lastest Price from Carfilzomib manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2020-05-13 Carfilzomib
868540-17-4
US $198.00 / mg 1g ≥98% 10kg BOC Sciences
2019-08-26 Carfilzomib
868540-17-4
US $0.00-0.00 / KG 1ASSAYS 99.0% 50kg/month Beijing Yibai Biotechnology Co., Ltd
2018-12-18 Carfilzomib
868540-17-4
US $7.00 / kg 1kg 99% 100KG career henan chemical co

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