ChemicalBook CAS DataBase List 75443-99-1

75443-99-1

Name	ACLARUBICIN HYDROCHLORIDE
CAS	75443-99-1
EINECS(EC#)	278-209-3
Molecular Formula	C42H54ClNO15
MDL Number	MFCD00133024
Molecular Weight	848.33
MOL File	75443-99-1.mol

Synonyms

aclacinon Aclarubicin HCl Aclarubicin hydrochlride ACLARUBICIN HYDROCHLORIDE aclacinomycinahydrochloride ACLARUBICIN HYDROCHLORIDE USP/EP/BP syl)oxy)-2,5,7-trihydroxy-,methylester,hydrochloride,(1r-(1-alpha,2-beta,4 n-2-yl)-alpha-l-lyxo-hexopyranosyl)-3-(dimethylamino)-alpha-l-lyxo-hexopyrano 1-Naphthacenecarboxylic acid, 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]-alpha-l-lyxo-hexopyranosyl]-3-(dimethylamino)-alpha-l-lyxo 1-Naphthacenecarboxylic acid, 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,6S)-tetrahydro-6-methyl-5-oxo-2H-pyran-2-yl]-α-L-lyxo-hexopyranosyl]-3-(dimethylamino)-α-L-lyxo-hexopyranosyl]oxy]-, meth 1-Naphthacenecarboxylic acid, 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]-, methyl ester, hydrochloride, [1R-(1α,2β,4β)]-

Chemical Properties

Melting point	151-153℃
Boiling point	898℃
Fp	>110°(230°F)
storage temp.	2-8°C
solubility	Soluble in DMSO or DMF at 25mg/ml
form	Solid
color	Light yellow to yellow

Safety Data

Hazard Codes	T
Risk Statements	23/24/25 less more
Safety Statements	36/37/39-45 less more
RIDADR	3249
RTECS	QI9283500
HazardClass	6.1(a)
PackingGroup	II

Hazard Information

Definition

ChEBI: Aclarubicin hydrochloride is an anthracycline.

Biological Activity

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 .

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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.

storage

4°C, protect from light

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