<Suppliers Price>

Aldoxorubicin•HCl

Names

[ CAS No. ]:
1361563-03-2

[ Name ]:
Aldoxorubicin•HCl

[Synonym ]:
S098K6HGD9
Aldoxorubicin hydrochloride
N'-[(1E)-1-{(2S,4S)-4-[(3-Amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-1,2,3,4,6,11-hexahydro-2-tetracenyl}-2-hydroxyethylidene]-6-(2,5-dioxo-2,5-dihydro -1H-pyrrol-1-yl)hexanehydrazide hydrochloride (1:1)
1H-Pyrrole-1-hexanoic acid, 2,5-dihydro-2,5-dioxo-, 2-[(1E)-1-[(2S,4S)-4-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-1,2,3,4,6,11-hexahydro-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-2-naphth acenyl]-2-hydroxyethylidene]hydrazide, hydrochloride (1:1)
MFCD25371995

Biological Activity

[Description]:

Aldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase
Signaling Pathways >> Antibody-drug Conjugate >> ADC Cytotoxin

[Target]

Topoisomerase II[4]


[In Vitro]

Aldoxorubicin hydrochloride (INNO-206)? (0.27 to 2.16 μM) inhibits blood vessel formation and reduces multiple myeloma cell growth in a pH-dependent fashion[1].

[In Vivo]

Aldoxorubicin hydrochloride (INNO-206) (10.8 mg/kg, i.v.) shows significantly smaller tumor volumes and IgG levels on days 28, and is well tolerated with 90% of mice surviving until the termination of the study in the mice bearing the LAGκ-1A tumor[1]. Aldoxorubicin hydrochloride (INNO-206) shows a good safety profile at doses up to 260 mg/mL doxorubicin equivalents, and is able to induce tumor regressions in breast cancer, small cell lung cancer and sarcoma in phase I study[2]. Aldoxorubicin hydrochloride (INNO-206) shows superior activity over doxorubicin in a murine renal cell carcinoma model and in breast carcinoma xenograft models[3].

[References]

[1]. Walker L, et al. Cell penetrating peptides fused to a thermally targeted biopolymer drug carrier improve the delivery and antitumor efficacy of an acid-sensitive doxorubicin derivative. Int J Pharm. 2012 Oct 15;436(1-2):825-32.  

[2]. Graeser R, et al. INNO-206, the (6-maleimidocaproyl hydrazone derivative of doxorubicin), shows superior antitumor efficacy compared to doxorubicin in different tumor xenograft models and in an orthotopic pancreas carcinoma model. Invest New Drugs. 2010 F  

[3]. Eric Sanchez, et al. Anti-Myeloma Effects of the Novel Anthracycline Derivative INNO-206. Clin Cancer Res.2012 18; 3856.

[4]. Kratz, F. INNO-206 (DOXO-EMCH), an Albumin-Binding Prodrug of Doxorubicin Under Development for Phase II Studies. Current Bioactive Compounds, 2011, 7(1): 33-38(6)

Chemical & Physical Properties

[ Molecular Formula ]:
C37H43ClN4O13

[ Molecular Weight ]:
787.21

[ Exact Mass ]:
786.251526

[ Appearance of Characters ]:
Powder

[ Storage condition ]:
store at -20℃ for one year(Powder)


Related Compounds