Tosedostat Struktur

Tosedostat

Bezeichnung:Tosedostat

CAS-Nr238750-77-1

Englisch Name:Tosedostat

CBNumberCB01518544

SummenformelC21H30N2O6

Molgewicht406.47

MOL-Datei238750-77-1.mol

Tosedostat physikalisch-chemischer Eigenschaften

Dichte	1.24
storage temp.	Keep in dark place,Sealed in dry,Store in freezer, under -20°C
Löslichkeit	≥40.6 mg/mL in DMSO; insoluble in H2O; ≥15.07 mg/mL in EtOH with ultrasonic
Aggregatzustand	A crystalline solid
pka	9.44±0.40(Predicted)
Farbe	White to off-white

Tosedostat Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Tosedostat is an inhibitor of aminopeptidases (IC₅₀s = 100, 150, and 220 nM for LAP, PUSA, and aminopeptidase N, respectively). It inhibits proliferation of human leukemia cell lines in vitro irrespective of p53, PTEN, or K-RAS mutational status (IC₅₀s = 10-770 nM). Tosedostat induces up-regulation of genes in amino acid transport and metabolic pathways and inhibits phosphorylation of mammalian target of rapamycin (mTOR) substrates in HL-60 cells, markers of amino acid depletion. In vivo, tosedostat (100 mg/kg) reduces total tumor burden and the number of spontaneous metastases in a mouse MDA-MB-435 xenograft model. Formulations containing tosedostat are under clinical investigation for the treatment of myeloid leukemia.
Verwenden
CHR-2797 is a novel metalloenzyme inhibitor that is converted into a pharmacological active acid product (CHR-79888) inside cells. CHR-2797 exerts antiproliferative effects against a range of tumor cell lines in vitro and in vivo and shows selectivity for transformed over nontransformed cells. Its antiproliferative effects are at least 300 times more potent than the prototypical aminopeptidase inhibitor, Bestatin.
Verwenden
Labelled Tosedostat nst a range of tumor cell lines in vitro and in vivo and shows selectivity for transformed over nontransformed cells. Its antiproliferative effects are at least 300 times more potent than the prototyp ical aminopeptidase inhibitor, Bestatin.
Definition
ChEBI: (2S)-2-[[(2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methyl-1-oxopentyl]amino]-2-phenylacetic acid cyclopentyl ester is a secondary carboxamide, a hydroxamic acid and a carboxylic ester.
Biologische Aktivität
Aminopeptidase inhibitor (IC 50 values are 100, 150, 220, > 1000, > 5000, > 10000 and > 30000 nM for LAP, PuSA, aminopeptidase N, aminopeptidase B, PILSAP, LTA 4 hydrolase and MetAP2 respectively). Potently inhibits tumor cell proliferation in a variety of tumor cell lines in vitro and in vivo .
Lager
Store at -20°C

Tosedostat Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

238750-77-1, Tosedostat Verwandte Suche:

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