1-Naphthacencarbonsure, 2-Ethyl-1,2,3,4,6,11-hexahydro-2,5,7-trihydroxy-6,11-dioxo-4-[[2,3,6-trideoxy-4-O-[2,6-dideoxy-4-O-[(2R-trans)-tetrahydro-6-methyl-5-oxo-2H-pyran-2-yl]-α-L-lyxo-hexopyranosyl]-3-(dimethylamino)-α-L-lyxo-hexopyranosyl]oxy]-, Methylester, Hydrochlorid, [1R-(1α,2β,4β)]-

Bezeichnung:1-Naphthacencarbonsure, 2-Ethyl-1,2,3,4,6,11-hexahydro-2,5,7-trihydroxy-6,11-dioxo-4-[[2,3,6-trideoxy-4-O-[2,6-dideoxy-4-O-[(2R-trans)-tetrahydro-6-methyl-5-oxo-2H-pyran-2-yl]-α-L-lyxo-hexopyranosyl]-3-(dimethylamino)-α-L-lyxo-hexopyranosyl]oxy]-, Methylester, Hydrochlorid, [1R-(1α,2β,4β)]-

CAS-Nr75443-99-1

Englisch Name:ACLARUBICIN HYDROCHLORIDE

CBNumberCB2189954

SummenformelC42H54ClNO15

Molgewicht848.33

MOL-Datei75443-99-1.mol

Synonyma

1-Naphthacencarbonsure, 2-Ethyl-1,2,3,4,6,11-hexahydro-2,5,7-trihydroxy-6,11-dioxo-4-[[2,3,6-trideoxy-4-O-[2,6-dideoxy-4-O-[(2R-trans)-tetrahydro-6-methyl-5-oxo-2H-pyran-2-yl]-α-L-lyxo-hexopyranosyl]-3-(dimethylamino)-α-L-lyxo-hexopyranosyl]oxy]-, Methylester, Hydrochlorid, [1R-(1α,2β,4β)]-

Schmelzpunkt	151-153℃
Siedepunkt	898℃
Flammpunkt	>110°(230°F)
storage temp.	2-8°C
Löslichkeit	Soluble in DMSO or DMF at 25mg/ml

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	23/24/25
S-Sätze:	36/37/39-45
RIDADR	3249
RTECS-Nr.	QI9283500
HazardClass	6.1(a)
PackingGroup	II

Gefahreninformationscode (GHS)

ACLARUBICIN HYDROCHLORIDE Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R23/24/25:Giftig beim Einatmen, Verschlucken und Berührung mit der Haut.
S-Sätze Betriebsanweisung:
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
Definition
ChEBI: Aclarubicin hydrochloride is an anthracycline.
Biologische Aktivität
Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) is a fluorescent molecule and the first non-peptidic inhibitor discovered to have discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome. It is also a dual inhibitor of topoisomerase I and II (topoisomerase I and II). It is an effective anthracycline chemotherapeutic agent for blood cancer and solid tumor related research.
in vitro

Aclacinomycin A could efficiently enter living cells and emit fluorescence in situ . Aclacinomycin A (10 μM for 15 min) is sufficient for clear detection of fluorescence in most of the cultured cells. Aclacinomycin A treatment (10 μM Acla for 15 min) results in approximately 20% dead (or nearly dead) cells.
Aclacinomycin A (Aclarubicin) effectively induces incorporation of exon 7 into SMN2 transcripts from the endogenous gene in type I SMA fibroblasts as well as into transcripts from a SMN2 minigene in the motor neuron cell line NSC34 .

in vivo

Aclarubicin hydrochloride(Aclacinomycin A) is very well absorbed in mice, rats, and dogs after its oral administration. The oral LD ₅₀ (76.5 mg/kg) is about twice the iv LD ₅₀ (35.6 mg/kg) in mice ^[4 .
Aclacinomycin A ( 0.75-6 mg/kg, ip daily) dose-dependently exhibits tumor growth in mice-based Leukemia P-388 model ^[4 .

td>

Animal Model:	DBA/2, CDF ₁ ( BALB/c×DBA/2) mice with Leukemia P-388 ^[4 .
Dosage:	0.75 mg/kg, 1.5 mg/kg, 3 mg/kg, 6 mg/kg.
Administration:	Intraperit oneal administration daily for 10 days starting 3 hr after transplantation.
Result:	Inhibited tumor growth.

target

20S proteasome.
Topoisomerase I and II.

1-Naphthacencarbonsure, 2-Ethyl-1,2,3,4,6,11-hexahydro-2,5,7-trihydroxy-6,11-dioxo-4-[[2,3,6-trideoxy-4-O-[2,6-dideoxy-4-O-[(2R-trans)-tetrahydro-6-methyl-5-oxo-2H-pyran-2-yl]-α-L-lyxo-hexopyranosyl]-3-(dimethylamino)-α-L-lyxo-hexopyranosyl]oxy]-, Methylester, Hydrochlorid, [1R-(1α,2β,4β)]- Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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