Carfilzomib
Based on 74 publication(s) in Google Scholar
Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 868540-17-4
- Formula: C40H57N5O7
- Molecular Weight:719.91
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Storage:Powder -20°C, 3 years , 4°C, 2 years
* The compound is unstable in solutions, freshly prepared is recommended.
Publications Citing Use of MedChemExpress (MCE) Carfilzomib
More- Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
- Nature. 2025 Feb;638(8050):519-527. [Abstract]
- Cancer Cell. 2024 Jul 8;42(7):1286-1300.e8. [Abstract]
- Drug Resist Updat. 2026 Jun 19:88:101436. [Abstract]
- Drug Resist Updat. 2024 Mar:73:101040. [Abstract]
- Nat Cell Biol. 2026 Apr;28(4):812-827. [Abstract]
- Mol Cell. 2023 Jan 19;83(2):281-297.e10. [Abstract]
- Nat Commun. 2026 May 13;17(1):4331. [Abstract]
- Nat Commun. 2020 Sep 4;11(1):4417. [Abstract]
- Acta Pharm Sin B. 2024 Aug;14(8):3493-3512. [Abstract]
- Adv Sci (Weinh). 2024 Dec 16:e2409895. [Abstract]
- Leukemia. 2025 Mar;39(3):720-733. [Abstract]
- Biomaterials. 2022 Oct:289:121800. [Abstract]
- Cell Discov. 2026 Feb 24;12(1):13. [Abstract]
- Cell Discov. 2025 Sep 30;11(1):80. [Abstract]
- Research (Wash D C). 2024 May 22:7:0380. [Abstract]
- Cell Rep Med. 2025 Apr 2:102053. [Abstract]
- Mater Today Bio. 2025 Mar 10:32:101649. [Abstract]
- Cancer Lett. 2026 Mar 12:218435. [Abstract]
- EMBO J. 2024 Nov;43(21):5057-5084. [Abstract]
- Free Radic Biol Med. 2023 Jul:203:86-101. [Abstract]
- NPJ Precis Oncol. 2025 Nov 21;9(1):373. [Abstract]
- Br J Pharmacol. 2026 May 28. [Abstract]
- Biomed Pharmacother. 2025 Sep:190:118368. [Abstract]
- Cell Chem Biol. 2021 Apr 15;28(4):503-514.e12. [Abstract]
- Cell Death Discov. 2025 Nov 17;11(1):532. [Abstract]
- Cell Rep. 2026 Jun 2;45(6).
- Cell Rep. 2026 Feb 18;45(3):116993. [Abstract]
- Cell Rep. 2025 Mar 26:115468. [Abstract]
- Arch Toxicol. 2025 Feb;99(2):729-744. [Abstract]
- Cell Rep. 2024 Dec 21;44(1):115094. [Abstract]
- J Med Chem. 2025 Dec 25;68(24):26405-26417. [Abstract]
- J Med Chem. 2024 May 9;67(9):7146-7157. [Abstract]
- J Med Chem. 2022 Jan 13;65(1):747-756. [Abstract]
- Antioxidants (Basel). 2024 May 30;13(6):671. [Abstract]
- Elife. 2019 Mar 25:8:e45457. [Abstract]
- J Agric Food Chem. 2017 Jun 7;65(22):4384-4394. [Abstract]
- Eur J Med Chem. 2021 Jul 5:219:113455. [Abstract]
- Biochem Pharmacol. 2024 Jan:219:115939. [Abstract]
- Biochem Pharmacol. 2018 Oct:156:511-523. [Abstract]
- Mol Cancer Ther. 2017 Dec;16(12):2862-2870. [Abstract]
- Mol Cell Proteomics. 2017 Apr;16(4 suppl 1):S144-S160. [Abstract]
- Cells. 2026 May 1;15(9):831. [Abstract]
- Protein Sci. 2024 Dec;33(12):e5225. [Abstract]
- Cells. 2021 Dec 6;10(12):3431. [Abstract]
- Life Sci. 2025 May 20:123749. [Abstract]
- Life Sci. 2023 Dec 15:335:122245. [Abstract]
- Pharmaceuticals (Basel). 2024 Aug 20;17(8):1089. [Abstract]
- Eur J Pharmacol. 2025 Dec 5:1008:178303. [Abstract]
- Mol Oncol. 2026 Jun 5. [Abstract]
- Mol Pharm. 2026 Feb 16. [Abstract]
- Antimicrob Agents Chemother. 2025 Dec 10;69(12):e0089325. [Abstract]
- Mol Pharm. 2024 Oct 7;21(10):5192-5204. [Abstract]
- Mol Oncol. 2024 Jun;18(6):1552-1570. [Abstract]
- J Cell Mol Med. 2026 Apr;30(7):e71101. [Abstract]
- iScience. 2026 Feb 18;29(3).
- J Biol Chem. 2026 Jan 20:111182. [Abstract]
- Sci Rep. 2025 Feb 5;15(1):4395. [Abstract]
- J Virol. 2025 May 22:e0034725. [Abstract]
- Cytokine. 2025 Dec 3:197:157083. [Abstract]
- Cancer Med. 2026 Jun;15(6):e71985. [Abstract]
- J Cell Biochem. 2021 Jun;122(6):667-678. [Abstract]
- Fungal Genet Biol. 2021 Dec:157:103632. [Abstract]
- Oncol Lett. 2025 Mar 4;29(4):208. [Abstract]
- bioRxiv. 2026 Jun 26.
- bioRxiv. 2026 May 14:2026.05.12.724395. [Abstract]
- Charles University. 2026.
- Seoul National University. 2027.
- bioRxiv. 2025 July 04.
- bioRxiv. 2025 Jul 12:2025.07.08.663754. [Abstract]
- bioRxiv. 2025 Jun 24:2025.06.18.660465. [Abstract]
- bioRxiv. 2024 July 19.
- University of Pardubice. 2023 May 5.
- Research Square Print. 2023 Feb 3.
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Cell Proliferation/Viability Assay
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RT-PCR
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Histological Imaging/Staining
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WB
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WB
Biological Activity
IC50: 5 nM (Proteasome)
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
23.8 nM
Compound: Carfilzomib
|
Antiproliferative activity against human A431 cells after 72 hrs by oxyluciferin luminescence assay
Antiproliferative activity against human A431 cells after 72 hrs by oxyluciferin luminescence assay
|
[PMID: 26231162] |
| A549 | IC50 |
43.3 nM
Compound: Carfilzomib
|
Antiproliferative activity against human A549 cells after 72 hrs by MTS assay
Antiproliferative activity against human A549 cells after 72 hrs by MTS assay
|
[PMID: 30639896] |
| ARPE-19 | IC50 |
0.058 μM
Compound: Carfilzomib
|
Cytotoxicity against human ARPE-19 cells assessed as reduction in cell viability incubated for 96 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay
Cytotoxicity against human ARPE-19 cells assessed as reduction in cell viability incubated for 96 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay
|
[PMID: 38636481] |
| CCRF-CEM | IC50 |
6.1 nM
Compound: Carfilzomib
|
Antiproliferative activity against human CCRF-CEM cells after 72 hrs by oxyluciferin luminescence assay
Antiproliferative activity against human CCRF-CEM cells after 72 hrs by oxyluciferin luminescence assay
|
[PMID: 26231162] |
| HCT-116 | IC50 |
19.3 nM
Compound: Carfilzomib
|
Antiproliferative activity against human HCT116 cells after 72 hrs by oxyluciferin luminescence assay
Antiproliferative activity against human HCT116 cells after 72 hrs by oxyluciferin luminescence assay
|
[PMID: 26231162] |
| HCT-116 | IC50 |
9.6 nM
Compound: Carfilzomib
|
Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay
Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay
|
[PMID: 30639896] |
| HEK293 | IC50 |
92.1 μM
Compound: Kyprolis(R)
|
Inhibition of human ERG in HEK293 cells assessed as effect on QT interval
Inhibition of human ERG in HEK293 cells assessed as effect on QT interval
|
[PMID: 31383629] |
| LP-1 | IC50 |
22.7 nM
Compound: Carfilzomib
|
Antiproliferative activity against human LP-1 cells after 72 hrs by MTS assay
Antiproliferative activity against human LP-1 cells after 72 hrs by MTS assay
|
[PMID: 30639896] |
| MCF7 | IC50 |
0.0041 μM
Compound: Cfz
|
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
|
[PMID: 30165344] |
| MDA-MB-231 | IC50 |
0.0044 μM
Compound: Cfz
|
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
|
[PMID: 30165344] |
| MES-SA | IC50 |
18 nM
Compound: 2
|
Cytotoxicity against human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 19348473] |
| MES-SA | IC50 |
413 nM
Compound: 2
|
Cytotoxicity against multidrug resistance transporter expressing doxorubicin resistant human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against multidrug resistance transporter expressing doxorubicin resistant human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 19348473] |
| MGC-803 | IC50 |
934 nM
Compound: Carfilzomib
|
Antiproliferative activity against human MGC803 cells after 72 hrs by MTS assay
Antiproliferative activity against human MGC803 cells after 72 hrs by MTS assay
|
[PMID: 30639896] |
| MM1.S | IC50 |
<1 nM
Compound: 2
|
Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay
Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay
|
[PMID: 30611983] |
| MM1.S | IC50 |
1.5 nM
Compound: Carfilzomib
|
Antiproliferative activity against human MM1S cells measured after 72 hrs by MTS assay
Antiproliferative activity against human MM1S cells measured after 72 hrs by MTS assay
|
[PMID: 27765408] |
| MM1.S | IC50 |
1.5 nM
Compound: Carfilzomib
|
Cytotoxicity against human MM1S cells measured after 72 hrs by MTS assay
Cytotoxicity against human MM1S cells measured after 72 hrs by MTS assay
|
[PMID: 28027531] |
| MM1.S | IC50 |
14.35 nM
Compound: Carfilzomib
|
Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 33223460] |
| MM1.S | IC50 |
2.3 nM
Compound: Carfilzomib
|
Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay
Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay
|
[PMID: 30639896] |
| MOLT-4 | IC50 |
5.1 nM
Compound: 2
|
Inhibition of chymotrypsin-like activity of 20S proteasome in human MOLT4 cells after 1 hr by CellTiter-Glo luminescent assay
Inhibition of chymotrypsin-like activity of 20S proteasome in human MOLT4 cells after 1 hr by CellTiter-Glo luminescent assay
|
[PMID: 19348473] |
| NCI-H23 | IC50 |
0.018 μM
Compound: Cfz
|
Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
|
[PMID: 30964987] |
| NCI-H727 | IC50 |
0.6102 μM
Compound: Cfz
|
Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
|
[PMID: 30964987] |
| NCI-H929 | IC50 |
116.1 nM
Compound: Carfilzomib
|
Antiproliferative activity against human NCI-H929 cells after 72 hrs by MTS assay
Antiproliferative activity against human NCI-H929 cells after 72 hrs by MTS assay
|
[PMID: 30639896] |
| NCI-H929 | IC50 |
13.9 nM
Compound: Carfilzomib
|
Antiproliferative activity against human NCI-H929 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H929 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 33223460] |
| NCI-H929 | IC50 |
21.32 nM
Compound: Carfilzomib
|
Cytotoxic activity against human NCI-H929 cells after 72 hrs by MTS assay
Cytotoxic activity against human NCI-H929 cells after 72 hrs by MTS assay
|
[PMID: 24767818] |
| PC-3 | IC50 |
23.9 nM
Compound: Carfilzomib
|
Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay
Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay
|
[PMID: 30639896] |
| RKO | IC50 |
27.1 nM
Compound: Carfilzomib
|
Antiproliferative activity against human RKO cells after 72 hrs by oxyluciferin luminescence assay
Antiproliferative activity against human RKO cells after 72 hrs by oxyluciferin luminescence assay
|
[PMID: 26231162] |
| RPMI-8226 | IC50 |
0.0067 μM
Compound: Cfz
|
Cytotoxicity against human RPMI8226 cells after 48 hrs by MTT assay
Cytotoxicity against human RPMI8226 cells after 48 hrs by MTT assay
|
[PMID: 30165344] |
| RPMI-8226 | IC50 |
0.007 μM
Compound: Cfz
|
Cytotoxicity against human RPMI8226 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
Cytotoxicity against human RPMI8226 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
|
[PMID: 30964987] |
| RPMI-8226 | IC50 |
13.19 nM
Compound: Carfilzomib
|
Cytotoxic activity against human RPMI8226 cells after 72 hrs by MTS assay
Cytotoxic activity against human RPMI8226 cells after 72 hrs by MTS assay
|
[PMID: 24767818] |
| RPMI-8226 | IC50 |
13.2 nM
Compound: Carfilzomib
|
Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by MTS assay
Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by MTS assay
|
[PMID: 27765408] |
| RPMI-8226 | IC50 |
13.2 nM
Compound: Carfilzomib
|
Cytotoxicity against human RPMI8226 cells measured after 72 hrs by MTS assay
Cytotoxicity against human RPMI8226 cells measured after 72 hrs by MTS assay
|
[PMID: 28027531] |
| RPMI-8226 | IC50 |
14.1 nM
Compound: Carfilzomib
|
Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 33223460] |
| RPMI-8226 | IC50 |
2 nM
Compound: 2
|
Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay
Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay
|
[PMID: 30611983] |
| RPMI-8226 | IC50 |
2.1 nM
Compound: Carfilzomib
|
Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay
Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay
|
[PMID: 30639896] |
| RPMI-8226 | IC50 |
39.1 nM
Compound: Kyprolis(R)
|
Cytotoxicity against human RPMI8226 cells assessed as cell viability measured after 72 hrs by celltiter96 aqueous cell proliferation assay
Cytotoxicity against human RPMI8226 cells assessed as cell viability measured after 72 hrs by celltiter96 aqueous cell proliferation assay
|
[PMID: 31383629] |
| TOV21G | IC50 |
23.8 nM
Compound: Carfilzomib
|
Antiproliferative activity against human TOV21G cells after 72 hrs by oxyluciferin luminescence assay
Antiproliferative activity against human TOV21G cells after 72 hrs by oxyluciferin luminescence assay
|
[PMID: 26231162] |
| U-266 | IC50 |
35.7 nM
Compound: Kyprolis(R)
|
Cytotoxicity against human U266B1 cells assessed as cell viability measured after 72 hrs by celltiter96 aqueous cell proliferation assay
Cytotoxicity against human U266B1 cells assessed as cell viability measured after 72 hrs by celltiter96 aqueous cell proliferation assay
|
[PMID: 31383629] |
Carfilzomib displays preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, with over 80% inhibition at doses of 10 nM and above and little or no effect on the PGPH and T-L activities at doses up to 100 nM. Carfilzomib decreases the viability of ANBL-6, RPMI 8226 cells, U266 and KAS-6/1 cells with an IC50 less than 5 nM. Carfilzomib overcome Dex resistance, in that MM1.R cells reveals an IC50 of 15.2 nM, less than the value of 29.3 nM for parental MM1.S cells[1]. Co-treatment with carfilzomib and HDACIs leads to synergistic induction of cell death in various mantle cell lymphoma lines and primary mantle cell lymphoma cells. Combined treatment with carfilzomib or ONX0912 with vorinostat in HF-4B and Granta cells sharply increases caspase activation, PARP cleavage, JNK activation, MnSOD2 induction, and DNA damage[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.
Carfilzomib (2.0 mg/kg, i.v.) in conbination with 70 mg/kg vorinostat virtually abrogates tumor growth in Granta-luciferace cell xenograft flank model. Combined treatment results in a pronounced reduction in bioluminescence compared to animals treated with single agents or controls with minimal toxicity[2].
Carfilzomib can be used in animal models to construct models of cardiotoxicity and hypertension.
Administration: 8 mg/kg • i.p. • once every two days for 6 days
Administration: 8 mg/kg • i.p. • once every 2 days for 7 days
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 868540-17-4
-
Appearance Solid
-
Molecular Weight 719.91
-
Formula C40H57N5O7
-
Color White to off-white
-
SMILES
C[C@@]1(C([C@H](CC(C)C)NC([C@@H](NC([C@H](CC(C)C)NC([C@@H](NC(CN2CCOCC2)=O)CCC3=CC=CC=C3)=O)=O)CC4=CC=CC=C4)=O)=O)OC1
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Synonyms
PR-171
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years * The compound is unstable in solutions, freshly prepared is recommended.
Publications (74)
-
Journal Impact Factor
-
Most Recent
-
Signal Transduct Target Ther
Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]2025 Dec 15;10(1):406. PMID: 41392286 -
Nature
2025 Feb;638(8050):519-527. PMID: 39880951 -
Cancer Cell
Anti-tumor efficacy of HRS-4642 and its potential combination with proteasome inhibition in KRAS G12D-mutant cancer. [Abstract]2024 Jul 8;42(7):1286-1300.e8. PMID: 38942026
Carfilzomib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 Jul 8;42(7):1286-1300.e8. [Abstract]
KP-1 cells were treated with vehicle, Carfilzomib (200 nM; 48 h) for 48 h. Ifi30, Irf7, Ddx60 expression levels are assessed using RT-PCR.
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Drug Resist Updat
NHE6-driven endosome-autophagy axis confers proteasome inhibitor resistance in multiple myeloma. [Abstract]2026 Jun 19:88:101436. PMID: 42349083 -
Drug Resist Updat
NDRG1 overcomes resistance to immunotherapy of pancreatic ductal adenocarcinoma through inhibiting ATG9A-dependent degradation of MHC-1. [Abstract]2024 Mar:73:101040. PMID: 38228036 -
Nat Cell Biol
TOLLIP targets GSDME-NT-carrying endocytic vesicles for autophagy to regulate pyroptosis and chemotherapy efficacy. [Abstract]2026 Apr;28(4):812-827. PMID: 41803502 -
Mol Cell
Palmitoylation prevents sustained inflammation by limiting NLRP3 inflammasome activation through chaperone-mediated autophagy. [Abstract]2023 Jan 19;83(2):281-297.e10. PMID: 36586411 -
Nat Commun
Targeted degradation of USP7 in solid cancer cells reveals distinct effects of deubiquitinase degraders and inhibitors. [Abstract]2026 May 13;17(1):4331. PMID: 42129197 -
Nat Commun
Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease. [Abstract]2020 Sep 4;11(1):4417. PMID: 32887884 -
Acta Pharm Sin B
Phenylalanine deprivation inhibits multiple myeloma progression by perturbing endoplasmic reticulum homeostasis. [Abstract]2024 Aug;14(8):3493-3512. PMID: 39220878 -
Adv Sci (Weinh)
Targeted Delivery of c(RGDfk)-Modified Liposomes to Bone Marrow Through In Vivo Hitchhiking Neutrophils for Multiple Myeloma Therapy. [Abstract]2024 Dec 16:e2409895. PMID: 39679804 -
Leukemia
2025 Mar;39(3):720-733. PMID: 39885295 -
Biomaterials
2022 Oct:289:121800. PMID: 36166893 -
Cell Discov
ASCT2 palmitoylation regulated by JNK1-ZDHHC14 axis orchestrates glutamine metabolism and NSCLC progression. [Abstract]2026 Feb 24;12(1):13. PMID: 41730846 -
Cell Discov
2025 Sep 30;11(1):80. PMID: 41027888 -
Research (Wash D C)
USP18 Antagonizes Pyroptosis by Facilitating Selective Autophagic Degradation of Gasdermin D. [Abstract]2024 May 22:7:0380. PMID: 38779488 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 2:102053. PMID: 40187357 -
Mater Today Bio
Enhanced anticancer effect of carfilzomib by codelivery of calcium peroxide nanoparticles targeting endoplasmic reticulum stress. [Abstract]2025 Mar 10:32:101649. PMID: 40160245 -
Cancer Lett
Identification of the MRTFA/SRF pathway as a critical regulator of quiescence and chemotherapy resistance in cancer. [Abstract]2026 Mar 12:218435. PMID: 41831517 -
EMBO J
2024 Nov;43(21):5057-5084. PMID: 39284914 -
Free Radic Biol Med
Targeting ABCB6 with nitidine chloride inhibits PI3K/AKT signaling pathway to promote ferroptosis in multiple myeloma. [Abstract]2023 Jul:203:86-101. PMID: 37044150 -
NPJ Precis Oncol
Integrative profiling strategies to guide personalized therapy in mantle cell lymphoma: a pilot study. [Abstract]2025 Nov 21;9(1):373. PMID: 41272086 -
Br J Pharmacol
Shared and specific molecular mechanisms of proteasome inhibitors in chemotherapy-induced peripheral neurotoxicity. [Abstract]2026 May 28. PMID: 42206739 -
Biomed Pharmacother
Increased cellular uptake and proteasome inhibition of carfilzomib through the optimized self-nanoemulsifying drug delivery system. [Abstract]2025 Sep:190:118368. PMID: 40680669
Carfilzomib purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2025 Sep:190:118368. [Abstract]
Carfilzomib (0.1-1000 μM; 24 h). Cell viability of RPMI 8226 cells after treatment with raw CFZ (Carfilzomib) for 24 h.
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Cell Chem Biol
2021 Apr 15;28(4):503-514.e12. PMID: 33400925 -
Cell Death Discov
ChaC1-based drug screenings identify a synergistic lethal effect of auranofin and proteasome inhibitors in hepatocellular carcinoma cells. [Abstract]2025 Nov 17;11(1):532. PMID: 41249117 -
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Cell Rep
Small-molecule enhancement of METTL3 S-palmitoylation as a therapeutic strategy for osteoarthritis. [Abstract]2026 Feb 18;45(3):116993. PMID: 41719123 -
Cell Rep
2025 Mar 26:115468. PMID: 40168988 -
Arch Toxicol
Canagliflozin differentially modulates carfilzomib-induced endoplasmic reticulum stress in multiple myeloma and endothelial cells. [Abstract]2025 Feb;99(2):729-744. PMID: 39645617 -
Cell Rep
The N-degron pathway mediates the autophagic degradation of cytosolic mitochondrial DNA during sterile innate immune responses. [Abstract]2024 Dec 21;44(1):115094. PMID: 39709605 -
J Med Chem
α-Aminoboronic Acid Moieties in Boro Dipeptides Modulate Proteasome Subunit Selectivity and Provide Access to Compounds with Potent Anticancer and Anti-Inflammatory Activity. [Abstract]2025 Dec 25;68(24):26405-26417. PMID: 41344819 -
J Med Chem
Brain-Permeable Immunoproteasome-Targeting Macrocyclic Peptide Epoxyketones for Alzheimer's Disease. [Abstract]2024 May 9;67(9):7146-7157. PMID: 38636481 -
J Med Chem
2022 Jan 13;65(1):747-756. PMID: 34965125 -
Antioxidants (Basel)
Empagliflozin Alleviates Carfilzomib-Induced Cardiotoxicity in Mice by Modulating Oxidative Stress, Inflammatory Response, Endoplasmic Reticulum Stress, and Autophagy. [Abstract]2024 May 30;13(6):671. PMID: 38929110
Carfilzomib purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2024 May 30;13(6):671. [Abstract]
Carfilzomib (8 mg/kg; i.p.; 2 consecutive days). Photomicrographs presents histopathological alterations along the heart tissue sections among the studied groups (hematoxylin and eosin stain, magnification power = 400×, and scale bar = 50 µm). Sections from control mice and EMPA-alone-treated mice demonstrates standard myocardial fibers with intact myocytes (arrows). CFZ (Carfilzomib)-treated mice highlights degenerated and necrotic cardiomyocytes (circle), nuclear pyknosis (arrow), increase in intermuscular spaces (arrow with tail), hemorrhagic spots (star), infiltration of inflammatory cells (wave arrow), fat cells (arrowhead), and congested vasculatures (rectangle). EMPA + CFZ-treated mice discloses many apparent intact cardiomyocytes (arrow), scarce apoptotic cardiomyocytes (curvy arrow), and congested vasculatures (rectangle).
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Elife
Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models. [Abstract]2019 Mar 25:8:e45457. PMID: 30907729 -
J Agric Food Chem
Resveratrol Reactivates Latent HIV through Increasing Histone Acetylation and Activating Heat Shock Factor 1. [Abstract]2017 Jun 7;65(22):4384-4394. PMID: 28471170
Carfilzomib purchased from MedChemExpress. Usage Cited in: J Agric Food Chem. 2017 Jun 7;65(22):4384-4394. [Abstract]
Resveratrol activates the HSF1 signaling pathway. J-Lat A2 cells are treated with various concentrations of Resveratrol or Carfilzomib (50 nM) for 48 h. Then the cells are lysed and Ser320 phosphorylated HSF1 and total HSF1 are detected by Western blot with corresponding antibodies.
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Eur J Med Chem
2021 Jul 5:219:113455. PMID: 33894528 -
Biochem Pharmacol
Carfilzomib suppressed LDHA-mediated metabolic reprogramming by targeting ATF3 in esophageal squamous cell carcinoma. [Abstract]2024 Jan:219:115939. PMID: 38000560 -
Biochem Pharmacol
PR-957, a selective immunoproteasome inhibitor, reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1. [Abstract]2018 Oct:156:511-523. PMID: 30170098
Carfilzomib purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Oct:156:511-523. [Abstract]
J-Lat 10.6 cells are treated with DMSO, PR-957 (150 nM) or Carfilzomib (40 nM) alone with or without the HSF1 inhibitor KRIBB11 (1.25 µM) for 48 h. Then the cells are lysed, and Ser320 phosphorylated HSF1, total HSF1 and p24 are detected by Western blot with the corresponding antibodies.
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Mol Cancer Ther
CRISPR Genome-Wide Screening Identifies Dependence on the Proteasome Subunit PSMC6 for Bortezomib Sensitivity in Multiple Myeloma. [Abstract]2017 Dec;16(12):2862-2870. PMID: 28958990 -
Mol Cell Proteomics
Label-free Proteomic Analysis of Exosomes Derived from Inducible Hepatitis B Virus-Replicating HepAD38 Cell Line. [Abstract]2017 Apr;16(4 suppl 1):S144-S160. PMID: 28242843 -
Cells
MDM2 Drives Proteasome Inhibitor Resistance and Represents a TP53-Independent Therapeutic Vulnerability in Multiple Myeloma. [Abstract]2026 May 1;15(9):831. PMID: 42121932 -
Protein Sci
Distinct substrate specificities of the three catalytic subunits of the Trichomonas vaginalis proteasome. [Abstract]2024 Dec;33(12):e5225. PMID: 39589076 -
Cells
Fragment-Sized and Bidentate (Immuno)Proteasome Inhibitors Derived from Cysteine and Threonine Targeting Warheads. [Abstract]2021 Dec 6;10(12):3431. PMID: 34943940 -
Life Sci
PSME2 promotes malignant progression through autophagy modulation via IL-6/STAT3 signaling pathway in esophageal squamous cell carcinoma. [Abstract]2025 May 20:123749. PMID: 40404117 -
Life Sci
Lactoferrin ameliorates carfilzomib-induced renal and pulmonary deficits: Insights to the inflammasome NLRP3/NF-κB and PI3K/Akt/GSK-3β/MAPK axes. [Abstract]2023 Dec 15:335:122245. PMID: 37926296 -
Pharmaceuticals (Basel)
The Proteasome Inhibitor Marizomib Evokes Endoplasmic Reticulum Stress and Promotes Apoptosis in Human Glioblastoma Cells. [Abstract]2024 Aug 20;17(8):1089. PMID: 39204194 -
Eur J Pharmacol
Doxorubicin-mediated retardation of aggresome formation enhances Carfilzomib-induced cell death synergistically by augmenting ER stress and proapoptotic signaling. [Abstract]2025 Dec 5:1008:178303. PMID: 41183585 -
Mol Oncol
Patient therapy outcome modeling in cancer organoids is improved by cancer-associated fibroblasts and organoid assembly convolution. [Abstract]2026 Jun 5. PMID: 42246237 -
Mol Pharm
2026 Feb 16. PMID: 41699819 -
Antimicrob Agents Chemother
Inhibitors of the 20S proteasome β5 subunit as potent and selective agents against Trichomonas vaginalis. [Abstract]2025 Dec 10;69(12):e0089325. PMID: 41218108 -
Mol Pharm
Fabrication of Poly Lactic- co-Glycolic Acid Microneedles for Sustained Delivery of Lipophilic Peptide-Carfilzomib. [Abstract]2024 Oct 7;21(10):5192-5204. PMID: 39255036 -
Mol Oncol
2024 Jun;18(6):1552-1570. PMID: 38348572 -
J Cell Mol Med
2026 Apr;30(7):e71101. PMID: 41896195 -
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J Biol Chem
Andrographolide targets syndecan4 to impair its interaction with syntenin and inhibits the biogenesis of small extracellular vesicles. [Abstract]2026 Jan 20:111182. PMID: 41570990 -
Sci Rep
Identifying common pathways for doxorubicin and carfilzomib-induced cardiotoxicities: transcriptomic and epigenetic profiling. [Abstract]2025 Feb 5;15(1):4395. PMID: 39910168 -
J Virol
Palmitoylation enhances the stability of porcine epidemic diarrhea virus spike protein by antagonizing its degradation via chaperone-mediated autophagy to facilitate viral proliferation. [Abstract]2025 May 22:e0034725. PMID: 40401979 -
Cytokine
Drug repurposing for cytokine storm: baricitinib, ciclesonide, and acalabrutinib modulate cytokine release in a translational in vitro lymphoblastoid cell line model. [Abstract]2025 Dec 3:197:157083. PMID: 41344136 -
Cancer Med
Synergistic Antitumor Activity of HAT Inhibitor A485 and XPO1 Inhibitor KPT8602 in Multiple Myeloma. [Abstract]2026 Jun;15(6):e71985. PMID: 42231094 -
J Cell Biochem
Thioxothiazolidin derivative, 4-OST, inhibits melanogenesis by enhancing the specific recruitment of tyrosinase-containing vesicles to lysosome. [Abstract]2021 Jun;122(6):667-678. PMID: 33480093 -
Fungal Genet Biol
SsATG8 and SsNBR1 mediated-autophagy is required for fungal development, proteasomal stress response and virulence in Sclerotinia sclerotiorum. [Abstract]2021 Dec:157:103632. PMID: 34710583 -
Oncol Lett
Carfilzomib inhibits the progression of hepatocellular cancer by upregulating GADD45α expression. [Abstract]2025 Mar 4;29(4):208. PMID: 40070787 -
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bioRxiv
2026 May 14:2026.05.12.724395. PMID: 42182270 -
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bioRxiv
2025 Jul 12:2025.07.08.663754. PMID: 40672312 -
bioRxiv
2025 Jun 24:2025.06.18.660465. PMID: 40666929 -
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Solvent & Solubility
DMSO : 125 mg/mL (173.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (3.47 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * The compound is unstable in solutions, freshly prepared is recommended.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
WST-1 is used to determine the effects of proteasome inhibitors on cell proliferation according to the manufacturer's protocol. The inhibition of proliferation is calculated in relation to parallel control cells that receive vehicle alone and tabulated in KaleidaGraph 3.0.1 or Excel 2000. A linear spline function is used to interpolate the median inhibitory concentration (IC50) using XLfit 4 software. The degree of resistance (DOR) is calculated using the formula: DOR=IC50(resistant cells)/IC50(sensitive cells).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal studies are performed utilizing Beige-nude-XID mice. 10×106 Granta514 cells are pelleted, washed twice with 1X PBS, injected subcutaneously into the right flank. Once the tumors are visible, 5 to 6 mice are treated with carfilzomib±vorinostat and progress of tumor growth or regression is monitored. Stock vorinostat and carfilzomib is dissolved in DMSO and 10% sulfobutylether betacyclodextrin in 10 mM citrate buffer pH respectively. They are stored in −80°C in small aliquots and diluted before injection.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (288 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[2]. Yang J, et al. Pharmacokinetics, pharmacodynamics, metabolism, distribution, and excretion of carfilzomib in rats. Drug Metab Dispos. 2011 Oct;39(10):1873-82. [Content Brief]
[3]. Efentakis P, et al. Molecular mechanisms of carfilzomib-induced cardiotoxicity in mice and the emerging cardioprotective role of metformin. Blood. 2019 Feb 14;133(7):710-723. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.3891 mL | 6.9453 mL | 13.8906 mL | 34.7266 mL |
| 5 mM | 0.2778 mL | 1.3891 mL | 2.7781 mL | 6.9453 mL | |
| 10 mM | 0.1389 mL | 0.6945 mL | 1.3891 mL | 3.4727 mL | |
| 15 mM | 0.0926 mL | 0.4630 mL | 0.9260 mL | 2.3151 mL | |
| 20 mM | 0.0695 mL | 0.3473 mL | 0.6945 mL | 1.7363 mL | |
| 25 mM | 0.0556 mL | 0.2778 mL | 0.5556 mL | 1.3891 mL | |
| 30 mM | 0.0463 mL | 0.2315 mL | 0.4630 mL | 1.1576 mL | |
| 40 mM | 0.0347 mL | 0.1736 mL | 0.3473 mL | 0.8682 mL | |
| 50 mM | 0.0278 mL | 0.1389 mL | 0.2778 mL | 0.6945 mL | |
| 60 mM | 0.0232 mL | 0.1158 mL | 0.2315 mL | 0.5788 mL | |
| 80 mM | 0.0174 mL | 0.0868 mL | 0.1736 mL | 0.4341 mL | |
| 100 mM | 0.0139 mL | 0.0695 mL | 0.1389 mL | 0.3473 mL |