Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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C127870-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $58.90 | |
C127870-10mg | 10mg | In stock | $82.90 | |
C127870-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $124.90 | |
C127870-50mg | 50mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $165.90 | |
C127870-100mg | 100mg | In stock | $224.90 | |
C127870-500mg | 500mg | In stock | $1,012.90 |
Potent, irreversible proteasome inhibitor.
Synonyms | (alphaS)-alpha-[[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-3-ph |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | Carfilzomib, an irreversible proteasome inhibitor, has a favorable safety profile and significant anti-tumor activity in patients with relapsed and refractory multiple myeloma (MM). Here we summarize the clinical pharmacokinetics (PK), metabolism, and dru |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | 26S proteosome inhibitor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. |
ALogP | 4.7 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | (2S)-4-methyl-N-[(2S)-1-[[(2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]-4-phenylbutanoyl]amino]pentanamide |
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INCHI | InChI=1S/C40H57N5O7/c1-27(2)22-32(36(47)40(5)26-52-40)42-39(50)34(24-30-14-10-7-11-15-30)44-38(49)33(23-28(3)4)43-37(48)31(17-16-29-12-8-6-9-13-29)41-35(46)25-45-18-20-51-21-19-45/h6-15,27-28,31-34H,16-26H2,1-5H3,(H,41,46)(H,42,50)(H,43,48)(H,44,49)/t31-,32-,33-,34-,40+/m0/s1 |
InChi Key | BLMPQMFVWMYDKT-NZTKNTHTSA-N |
Canonical SMILES | CC(C)CC(C(=O)C1(CO1)C)NC(=O)C(CC2=CC=CC=C2)NC(=O)C(CC(C)C)NC(=O)C(CCC3=CC=CC=C3)NC(=O)CN4CCOCC4 |
Isomeric SMILES | CC(C)C[C@@H](C(=O)[C@]1(CO1)C)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC3=CC=CC=C3)NC(=O)CN4CCOCC4 |
PubChem CID | 11556711 |
Molecular Weight | 719.91 |
PubChem CID | 11556711 |
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CAS Registry No. | 868540-17-4 |
DrugBank Ligand | DB08889 |
ChEMBL Ligand | CHEMBL451887 |
Wikipedia | Carfilzomib |
DrugCentral Ligand | 4483 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
E2406051 | Certificate of Analysis | Mar 20, 2024 | C127870 |
F2208178 | Certificate of Analysis | Mar 20, 2024 | C127870 |
F2208180 | Certificate of Analysis | Mar 20, 2024 | C127870 |
F2208181 | Certificate of Analysis | Mar 20, 2024 | C127870 |
F2208243 | Certificate of Analysis | Mar 20, 2024 | C127870 |
B1525012 | Certificate of Analysis | Sep 13, 2022 | C127870 |
J2323084 | Certificate of Analysis | Mar 23, 2022 | C127870 |
Solubility | DMSO 50 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
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Pictogram(s) | GHS06, GHS08, GHS07 |
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Signal | Danger |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H413:May cause long lasting harmful effects to aquatic life H302:Harmful if swallowed H300:Fatal if swallowed H372:Causes damage to organs through prolonged or repeated exposure H361:Suspected of damaging fertility or the unborn child |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P271:Use only outdoors or in a well-ventilated area. P270:Do not eat, drink or smoke when using this product. P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing. P403+P233:Store in a well-ventilated place. Keep container tightly closed. P362+P364:Take off contaminated clothing and wash it before reuse. P330:Rinse mouth. P203:Obtain, read and follow all safety instructions before use. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P301+P316:IF SWALLOWED: Get emergency medical help immediately. P301+P317:IF SWALLOWED: Get medical help. P318:if exposed or concerned, get medical advice. P337+P317:If eye irritation persists: Get medical help. P332+P317:If skin irritation occurs: Get medical help. P319:Get medical help if you feel unwell. |
1. Hanada M, Sugawara K, Kaneta K, Toda S, Nishiyama Y, Tomita K, Yamamoto H, Konishi M, Oki T. (1992) Epoxomicin, a new antitumor agent of microbial origin.. J Antibiot, 45 (11): (1746-52). [PMID:1468981] [10.1021/op500134e] |
2. Kuhn DJ, Chen Q, Voorhees PM, Strader JS, Shenk KD, Sun CM, Demo SD, Bennett MK, van Leeuwen FW, Chanan-Khan AA et al.. (2007) Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma.. Blood, 110 (9): (3281-90). [PMID:17591945] [10.1021/op500134e] |
3. Wang ES et al.. (2021) Acute pharmacological degradation of Helios destabilizes regulatory T cells.. Nat Chem Biol, 17 (6): (711-717). [PMID:34035522] |