INNO-206是多柔比星的白蛋白结合前药,在酸性条件下从白蛋白中释放出来。 INNO-206在各种癌细胞系和小鼠肿瘤模型中具有有效的抗肿瘤活性。
Description | INNO-206 is an albumin-binding prodrug of doxorubicin, which is released from albumin under acidic conditions. INNO-206 has potent antitumor activities in various cancer cell lines and in in murine tumor models. | ||||||||||||||||
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IC50 & Target |
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In Vitro | 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 | 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]. 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]. INNO-206 shows superior activity over doxorubicin in a murine renal cell carcinoma model and in breast carcinoma xenograft models[3]. | ||||||||||||||||
Solvent & Solubility | In Vitro: 10 mM in DMSO Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. | ||||||||||||||||
References | |
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