CARFILZOMIB

Carfilzomib is a proteasome inhibitor inducing apoptosis in myeloma cells. Side effects include cardiotoxicity, thrombocytopenia, and fatigue. Only GMP materials will be supplied, logistics all according to GDP.

SKU: 6369683377bc Category: Tag:

Product Description


Mechanism of action

Carfilzomib is an irreversible proteasome inhibitor targeting the chymotrypsinlike activity of the 5 subunit of the 20S proteasome. It forms a covalent bond via its epoxyketone pharmacophore, blocking proteolytic degradation of ubiquitinated proteins. This leads to endoplasmicreticulum stress, impaired protein homeostasis, mitochondrial dysfunction and apoptosis in rapidly proliferating cells.

Benefits and advantages

Used in cancerbiology research, ubiquitinproteasome pathway studies, apoptosissignalling modelling, drugresistance mechanism analysis, multiplemyeloma models and proteostasis research. It serves as a reference irreversible proteasome inhibitor.

Side effects and risks

Risks include cardiotoxicity, hypertension, thrombocytopenia, neutropenia, infusion reactions, renal toxicity and peripheral neuropathy. Handle under full cytotoxicagent containment.

Only GMP materials will be supplied, logistics all according to GDP.

Datasheet


Molecular Formula

C40H57N5O7

Molecular Weight

719.9 g/mol

CAS Number

868540-17-4

Storage Condition

Store in a cool, dry place. Keep container tightly closed. Protect from moisture and light.

Solubility

Insoluble

Purity

Purity information is available upon request (COA).

Synonym

Carfilzomib; 868540-17-4; Kyprolis; PR-171; NSC-758252

IUPAC/Chemical 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

InChl Key

BLMPQMFVWMYDKT-NZTKNTHTSA-N

InChl Code

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

References

https://pubchem.ncbi.nlm.nih.gov/compound/11556711;

3D Conformer.

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