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DOXO-EMCH

现货
Catalog No.
A3372
doxorubicin的前药
组合的产品项目
规格价格库存 数量
20mg
¥ 4,130.00
Ship with 10-15 days
10mg
¥ 2,260.00
Ship with 10-15 days
50mg
¥ 7,740.00
Ship with 10-15 days
100mg
¥ 11,350.00
Ship with 10-15 days

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Background

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.

Chemical Properties

StorageStore at -20°C
M.Wt750.75
Cas No.151038-96-9
FormulaC37H42N4O13
SynonymsINNO-206;Doxorubicin-EMCH;INNO 206
SolubilitySoluble in DMSO
Chemical NameN-[(Z)-[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
SDFDownload SDF
Canonical SMILESCC1C(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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

人多发性骨髓瘤细胞系RPMI8226和U266

溶解方法

可溶于DMSO。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

0.27-2.16 mmol/L,48小时

应用

INNO-206以pH依赖的方式抑制血管形成并降低多发性骨髓瘤细胞生长。在RPMI8226细胞中,INNO-206以浓度和pH依赖性方式降低细胞活力。在pH5条件下,INNO-206(≥0.54 mmol/L)基本上消除了细胞活力。在MM1S细胞系中,INNO-206以浓度和pH依赖性方式抑制细胞生长。

动物实验 [1, 2]:

动物模型

异种移植LAGk-1A肿瘤及多发性骨髓瘤LAGk-2异种移植物的小鼠模型

给药剂量

静脉注射,10.8 mg/kg;1.8 mg/kg,每周3次;5.4 mg/kg,每周1次

应用

在携带LAGk-1A肿瘤的小鼠中,静脉注射10.8 mg/kg剂量INNO-206,每周一次,在第28、35和42天肿瘤体积和IgG水平显著减少。在携带LAGk-2的小鼠中,静脉注射1.8 mg/kg剂量的INNO -206,每周3次,肿瘤体积显著降低。静脉注射5.4 mg/kg剂量INNO-206,每周一次,肿瘤体积显著减小。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Sanchez E, Li M, Wang C, et al. Anti-myeloma effects of the novel anthracycline derivative INNO-206[J]. Clinical Cancer Research, 2012, 18(14): 3856-3867.

[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.

质量控制

质量控制和MSDS

批次:

化学结构

DOXO-EMCH