Identification | Back Directory | [Name]
INNO206 | [CAS]
1361644-26-9 | [Synonyms]
Aldoxorubicin Aldoxorubicin (INNO-206) Aldoxorubicin Aldoxorubicin N-[(E)-[1-[(2S,4S)-4-[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-3,4-dihydro-1H-tetracen-2-yl]-2-hydroxyethylidene]amino]-6-(2,5-dioxopyrrol-1-yl)hexanamide 1H-Pyrrole-1-hexanoic acid, 2,5-dihydro-2,5-dioxo-, (2E)-2-[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-naphthacenyl]-2-hydroxyethylidene]hydrazide (E)-N’-[1-[(2S,4S)-4-[[(2R,4S,5S,6S)-4-Amino-5-hydroxy-6-methyl-2-tetrahydropyranyl]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-1-pyrrolyl)hexanehydrazide | [Molecular Formula]
C37H42N4O13 | [MOL File]
1361644-26-9.mol | [Molecular Weight]
750.75 |
Chemical Properties | Back Directory | [density ]
1.60±0.1 g/cm3(Predicted) | [storage temp. ]
-80°, stored under nitrogen,unstable in solution, ready to use. | [solubility ]
DMSO : 75 mg/mL (99.90 mM) | [form ]
Solid | [pka]
7.36±0.60(Predicted) | [color ]
Purple to purplish red |
Hazard Information | Back Directory | [Uses]
Aldoxorubicin (INNO-206) is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models. | [Biological Activity]
Aldoxorubicin (INNO-206) is an albumin-bound prodrug of doxorubicin, a DNA topoisomerase II inhibitor, released from albumin under acidic conditions. It has potent antitumor activity in various cancer cell lines and mouse tumor models. | [in vitro]
Aldoxorubicin (INNO-206) (0.27 to 2.16 μM) inhibits blood vessel formation and reduces multiple myeloma cell growth in a pH-dependent fashion. | [in vivo]
Aldoxorubicin (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. | [target]
Topoisomerase II | Daunorubicins/Doxorubicins | | [IC 50]
Topoisomerase II; Daunorubicins/Doxorubicins | [storage]
-80°, stored under nitrogen,unstable in solution, ready to use. | [References]
[1] Eric Sanchez, et al. Anti-Myeloma Effects of the Novel Anthracycline Derivative INNO-206. Clin Cancer Res.2012 18; 3856. [2] 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) [3] 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 DOI:10.1007/s10637-008-9208-2 [4] 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. DOI:10.1016/j.ijpharm.2012.07.043 |
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BOC Sciences
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Musechem
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www.musechem.com |
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