General
Preferred name
CARFILZOMIB
Synonyms
PR-171 ()
Kyprolis ()
CT-CARF ()
A-1098 ()
Carfilzomib (PR-171) ()
NSC-758252 ()
Carfilzomib-d8 ()
P&D ID
PD004089
CAS
868540-17-4
1537187-53-3
Tags
nuisance
covalent binder
drug
available
Approved by
PMDA
FDA
First approval
2012
2009
Drug Status
investigational
approved
Drug indication
Multiple myeloma
Small-cell lung cancer
Max Phase
Phase 4
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
ABSORPTION
Cmax, single IV dose of 27 mg/m^2 = 4232 ng/mL; ; AUC, single IV dose of 27 mg/m^2 = 379 ng•hr/mL;; Carfilzomib does not accumulation in the systemic. At doses between 20 and 36 mg/m2, there was a dose-dependent increase in exposure.
TOXICITY
Most commonly reported adverse reactions (incidence ≥ 30%) are fatigue, anemia, nausea, thrombocytopenia, dyspnea, diarrhea, and pyrexia. The two dose limiting toxicities are thrombocytopenia and febrile neutropenia. ; Maximum tolerate dose = 15 mg/m^2
DESCRIPTION
Carfilzomib is a tetrapeptide analogue of epoxomicin, an Actinomycete derived selective proteasome inhibitor .
(GtoPdb)
DESCRIPTION
Potent and selective Src tyrosine kinase family inhibitor; anticancer; antiviral; orally bioavailable
(Tocris Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
16
Organisms
0
Compound Sets
28
AdooQ Bioactive Compound Library
ChEMBL Approved Drugs
ChEMBL Drugs
CovalentInDB
CovBinderInPDB
CBR000692
CBR000693
CBR000694
CBR000695
CBR000696
CBR000697
CBR000698
CBR000699
CBR000700
CBR000701
CBR000708
CBR000709
CBR000710
CBR000711
CBR000712
CBR000713
CBR000715
CBR000716
CBR000717
CBR000718
CBR001061
CBR001062
CBR001063
CBR001064
CBR001065
CBR001066
CBR001067
CBR001068
CBR001069
CBR001070
CBR001072
CBR001073
CBR001074
CBR001075
CBR002618
CBR002619
CBR002620
CBR002621
CBR002622
CBR003766
CBR003767
CBR003768
CBR003769
CBR003770
CBR003771
CBR003772
CBR003773
CBR003774
CBR003775
CBR003786
CBR003787
CBR003788
CBR003789
CBR003790
CBR003791
CBR003891
CBR003892
CBR003893
CBR003894
CBR003895
CBR003896
CBR005337
CBR005338
CBR005339
CBR005340
CBR005341
CBR005342
CBR005345
CBR005346
CBR005347
CBR005348
CBR005349
CBR005350
CBR005352
CBR005353
CBR005354
CBR005355
CBR005356
CBR005357
CBR005366
CBR005367
CBR005368
CBR005369
CBR005370
CBR005371
CBR005378
CBR005379
CBR005380
CBR005381
CBR005382
CBR005383
CBR005384
CBR005385
CBR005386
CBR005387
CBR005388
CBR005389
CBR005390
CBR005391
CBR005392
CBR005393
CBR005394
CBR005395
CBR005396
CBR005397
CBR005398
CBR005399
CBR005400
CBR005401
CBR005402
CBR005403
CBR005404
CBR005405
CBR005406
CBR005407
CBR005408
CBR005409
CBR005410
CBR005411
CBR005412
CBR005413
CBR005426
CBR005427
CBR005428
CBR005429
CBR005430
CBR005431
CBR005443
CBR005444
CBR005445
CBR005446
CBR005447
CBR005448
CBR005972
CBR005973
CBR005974
CBR005975
CBR005976
CBR006540
CBR006541
CBR006542
CBR006543
CBR006544
CBR006545
CBR006627
CBR006628
CBR006629
CBR006630
CBR006631
CBR006632
CBR006665
CBR006666
CBR006667
CBR006668
CBR006669
CBR006670
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
Natural product-based probes and drugs
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
Nuisance compounds in cellular assays
Reference compounds for characterizing cellular injury in high-content cellular morphology assays
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
38
Molecular Weight
719.43
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
4
Rotatable Bonds
20
Ring Count
4
Aromatic Ring Count
2
cLogP
2.58
TPSA
158.47
Fraction CSP3
0.57
Chiral centers
5.0
Largest ring
6.0
QED
0.15
Structural alerts
1
Protein disruption
Proteosome inhibition
Nuisance compounds in cellular assays
Related compounds
Custom attributes
(extracted from source data)
Pathway
Proteases/Proteasome
Ubiquitination
Apoptosis
Autophagy
Metabolic Enzyme/Protease
Target
Proteasome
PSMA1, PSMA2, PSMA3, PSMA4, PSMA5, PSMA6, PSMA7, PSMA8, PSMB1, PSMB10, PSMB11, PSMB2, PSMB3, PSMB4, PSMB5, PSMB6, PSMB7, PSMB8, PSMB9
Apoptosis related,Autophagy,COVID-19,Proteasome
MOA
Inhibitor
Proteasome inhibitor
Member status
member
Indication
multiple myeloma
Biosynthetic Origin
Peptide (NRPS)
Therapeutic Indication
Anticancer
Source data
