Carfilzomib


Catalog No. size PriceQuantity
M7161-2 2mg solid $83
M7161-10 10mg solid $324

Description

Cas:868540-17-4

Product Information:

Carfilzomib, also known as PR-171, is a tetrapeptide epoxyketone and an epoxomicin derivate with potential antineoplastic activity. Carfilzomib irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S proteasome, an enzyme 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 was approved by the FDA for use in patients with relapsed and refractory multiple myeloma on 20 July 2012.

 

Chemical Formula: C40H57N5O7

 

Exact Mass: 719.4258

 

Molecular Weight: 719.91

 

Elemental Analysis: C, 66.73; H, 7.98; N, 9.73; O, 15.56

 

Synonym:

 

PR171

PR-171

PR 171

Carflizomib

brand name: Kyprolis

 

Chemical Name: (S)-4-methyl-N-((S)-1-((S)-4-methyl-1-((R)-2-methyloxiran-2-yl)-1-oxopentan-2-ylamino)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamide

 

InChi Key: 

BLMPQMFVWMYDKT-NZTKNTHTSA-N

 

InChi 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

 

Smiles Code:

CC(C)C[C@H](NC([C@@H](NC(CN1CCOCC1)=O)CCC2=CC=CC=C2)=O)C(N[C@@H](CC3=CC=CC=C3)C(N[C@@H](CC(C)C)C([C@]4(C)OC4)=O)=O)=O.

 

 

Technical Data:

 

Appearance: white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

 

 

References

 

  1. Kim KB, Crews CM. From epoxomicin to carfilzomib: chemistry, biology, and medical outcomes. Nat Prod Rep. 2013 May;30(5):600-4. doi: 10.1039/c3np20126k. Review. PubMed PMID: 23575525; PubMed Central PMCID: PMC3815659. 

  1. Kortuem KM, Stewart AK. Carfilzomib. Blood. 2013 Feb 7;121(6):893-7. doi: 10.1182/blood-2012-10-459883. Review. PubMed PMID: 23393020.

  1. Thompson JL. Carfilzomib: a second-generation proteasome inhibitor for the treatment of relapsed and refractory multiple myeloma. Ann Pharmacother. 2013 Jan;47(1):56-62. doi: 10.1345/aph.1R561. Epub 2013 Jan 8. Review. PubMed PMID: 23300152.

  1. Carfilzomib (Kryprolis) for multiple myeloma. Med Lett Drugs Ther. 2012 Dec 24;54(1406):103-4. Review. PubMed PMID: 23282792.

  2. McCormack PL. Carfilzomib: in relapsed, or relapsed and refractory, multiple myeloma. Drugs. 2012 Oct 22;72(15):2023-32. doi: 10.2165/11209010-000000000-00000. Review. PubMed PMID: 22994535.

 

Products are for research use only. Not for human use.

 

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