Carfilzomib
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- CAS-Nr.
- 868540-17-4
- Englisch Name:
- Carfilzomib
- Synonyma:
- PR 171;CS-603;Carfezomil;Carfilzomib;PR171;PR 171;Carfilzomib API;CarfilzoMib salt;CarfilzoMib/PR 171;Carfilzomib, >=99%;PR-171 (CarfilzoMib)
- CBNumber:
- CB12520831
- Summenformel:
- C40H57N5O7
- Molgewicht:
- 719.92
- MOL-Datei:
- 868540-17-4.mol
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Carfilzomib Eigenschaften
- Schmelzpunkt:
- 204 - 208°C
- Siedepunkt:
- 975.6±65.0 °C(Predicted)
- Dichte
- 1.161
- Flammpunkt:
- 543.8℃
- storage temp.
- -20°
- Löslichkeit
- Soluble in DMSO (up to 80 mg/ml) or in Ethanol (up to 25 mg/ml).
- Aggregatzustand
- solid
- pka
- 13.17±0.46(Predicted)
- Farbe
- White
- Stabilität:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 week.
- CAS Datenbank
- 868540-17-4
Sicherheit
- Risiko- und Sicherheitserklärung
- Gefahreninformationscode (GHS)
Bildanzeige (GHS) |
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Alarmwort |
Warnung |
Gefahrenhinweise |
Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
H302 |
Gesundheitsschädlich bei Verschlucken. |
Akute Toxizität oral |
Kategorie 4 |
Warnung |
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P264, P270, P301+P312, P330, P501 |
H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P302+P352, P321,P332+P313, P362 |
H319 |
Verursacht schwere Augenreizung. |
Schwere Augenreizung |
Kategorie 2 |
Warnung |
src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P305+P351+P338,P337+P313P |
H335 |
Kann die Atemwege reizen. |
Spezifische Zielorgan-Toxizität (einmalige Exposition) |
Kategorie 3 (Atemwegsreizung) |
Warnung |
src="/GHS07.jpg" width="20" height="20" /> |
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Sicherheit |
P261 |
Einatmen von Staub vermeiden. |
P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen. |
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Carfilzomib Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
In July 2012, the US FDA approved carfilzomib (also referred to as PR-171) for the treatment of patients with multiple myeloma (MM) who have received at least two prior therapies including bortezomib and an immunomodulatory agent and have demonstrated disease progression within 60 days of completion of the last therapy. Carfilzomib binds to and irreversibly inhibits the chymotrypsin-like protease activity of the constitutive proteosome (β5) and immunoproteosome (β5i) via its epoxyketone pharmacophore. Proteosome inhibition results in the accumulation of polyubiquitinated proteins and induction of apoptosis through activation of both the intrinsic and extrinsic caspase pathways. Carfilzomib inhibits chymotrypsin activity with an IC
50 of 6 nM and is less potent an inhibitor of trypsin and caspase (IC
50s of 3600 and 2400 nM, respectively). Cell cycle arrest and apoptosis are seen in a variety of hematologic and solid tumor cell lines (e.g.,MM, acutemyeloid leukemia (AML), pancreatic cancer, lung cancer) treated with carfilzomib.
Chemische Eigenschaften
White Solid
Verwenden
Carfilzomib is a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma.
Definition
ChEBI: Carfilzomib is a synthetic tetrapeptide consisting of morpholin-4-acetyl, L-2-amino-4-phenylbutanoyl, L-leucyl and L-phenylalanyl residues joined in sequence with the C-terminus connected to the amino group of (2<element S)-2-amino-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-1-one via an amide linkage. Used for the treatment of patients with multiple myeloma.
Clinical Use
Carfilzomib is an irreversible inhibitor of the chymotrypsin-like protease in the proteasome and was
approved in the U.S. for the treatment of multiple myeloma. Carfilzomib was discovered by
Proteolix which was later acquired by Onyx Therapeutics who completed the development of this drug.
Carfilzomib is also undergoing clinical evaluation for additional oncology indications such as relapsed
solid tumors, lymphoma, prolymphocytic leukemia, acute myeloid leukemia and acute lymphocytic leukemia.
Carfilzomib Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Carfilzomib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.
Global( 347)Lieferanten
868540-17-4()Verwandte Suche:
- CarfilzoMib salt
- CarfilzoMib/PR 171
- PR 171
- PR-171 (CarfilzoMib)
- (alphaS)-alpha-[(4-Morpholinylacetyl)amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-L-phenylalaninamide
- Carfilzomib
- CarfilzoMib, Free Base, >99%
- (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
- L-Phenylalaninamide, (αS)-α-[[2-(4-morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-
- (alphaS)-alpha-[(4-Morpholinylacetyl)amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-L-phenylalaninamide Carfilzomib(PR171)
- Carfilzomib (alphaS)-alpha-[(4-Morpholinylacetyl)amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-L-phenylalaninamide
- Carfilzomib, >=99%
- (αS)-α-[[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
- N-{(2S)-2-[(Morpholin-4-ylacetyl)aMino]-4-phenylbutanoyl}-L-leucyl-N-{(2S)-4-Methyl-1-[(2R)-2-Methyloxiran-2-yl]-1-oxopentan-2-yl}-L-phenylalaninaMide
- Carfilzomib API and intermediates
- Carfilzomib, 99%, irreversible proteasome inhibitor
- PR171;PR 171
- CS-603
- Carfilzomib API
- Carfilzomib (2R,4S)-Diol (7R)-Isomer
- Carfilzomib (2S,4S)-Diol (7R)-Isomer
- Carfilzomib (2S,4R)-Diol (7R)-Isomer
- Carfilzomib (2R,4R)-Diol (7R)-Isomer
- (S)-4-Methyl-N-[(S)-1-[[(S)-4-methyl-1-[(R)-2-methyloxiran-2-yl]-1-oxo-2-pentyl]amino]-1-oxo-3-phenyl-2-propyl]-2-[(S)-2-(2-morpholinoacetamido)-4-phenylbutanamido]pentanamide
- 7(R)-epi Carfilzomib (2R,4S)-diolQ: What is
7(R)-epi Carfilzomib (2R,4S)-diol Q: What is the CAS Number of
7(R)-epi Carfilzomib (2R,4S)-diol
- 7(R)-epi Carfilzomib (2S,4R)-diolQ: What is
7(R)-epi Carfilzomib (2S,4R)-diol Q: What is the CAS Number of
7(R)-epi Carfilzomib (2S,4R)-diol
- L-Phenylalaninamide, (αS)-α-[[2-(4-morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]- (Carfilzomib impurity)
- (αS)-α-[[2-(4-Morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-L-phenylalaninamide
- Carfilzomib(For R & D only)
- Carfezomil
- 868540-17-4
- 86854-17-4
- C40H57N5O7
- Inhibitors
- peptides
- API
- Inhibitor
- Pharmaceutical
- 868540-17-4
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