DOXO-EMCH

Short Summary : Prodrug of doxorubicin

Category : DNA Damage/DNA Repair|Topoisomerase

Purity : 0.98

CAS Number : 151038-96-9

Formula : C37H42N4O13

Molecular Weight : 750.75

SMILE : CC1C(C(CC(O1)OC2CC(CC3=C(C4=C(C(=C23)O)C(=O)C5=C(C4=O)C=CC=C5OC)O)(C(=NNC(=O)CCCCCN6C(=O)C=CC6=O)CO)O)N)O

Solubility : DMSO

Storage : Store at -20°C

Description : The (6-maleimidocaproyl) hydrazone derivative of doxorubicin (INNO-206), formerly known as DOXO-EMCH, is a prodrug of the anticancer agent doxorubicin which selectively binds to the cys34 of circulating albumin and accumulates in solid tumors due to passive targeting[1]. INNO-206 shows significantly superior antitumor efficacy over free doxorubicin in a spectrum of preclinical tumor models [2].In vivo: In a murine renal cell carcinoma model and in breast carcinoma xenograft models, INNO-206 has shown superior activity over doxorubicin. INNO-206 has shown more potent antitumor efficacy than free doxorubicin in the tumor models and is thus a promising clinical candidate for treating a broad range of solid tumors [2].Clinical trials: In a phase I study, INNO-206 showed a good safety profile at doses up to 260 mg/m2 doxorubicin equivalents. INNO-206 was able to induce tumor regressions in breast cancer, small cell lung cancer and sarcoma. [1].References:[1]. Kratz F. DOXO-EMCH (INNO-206): the first albumin-binding prodrug of doxorubicin to enter clinical trials[J]. Expert opinion on investigational drugs, 2007, 16(6): 855-866.[2]. Graeser R, Esser N, Unger H, 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[J]. Investigational new drugs, 2010, 28(1): 14-19.[3]. Graeser R, Esser N, Unger H, 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[J]. Investigational new drugs, 2010, 28(1): 14-19.

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