DOXO-EMCH
(Synonyms: INNO-206;Doxorubicin-EMCH;INNO 206) 目录号 : GC15250
Prodrug of doxorubicin
Cas No.:151038-96-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
-
Purity > 98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Human multiple myeloma cell lines RPMI8226 and U266 |
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Preparation method |
Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.27-2.16 mmol/L, 48 hours |
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Applications |
INNO-206 inhibited blood vessel formation and reduced multiple myeloma cell growth in a pH-dependent fashion. In RPMI8226 cells, INNO-206 decreased cell viability in concentration-and pH-dependent manner. At pH5, INNO-206（≥0.54 mmol/L）essentially eliminated cell viability. In the MM1S cell line, INNO-206 inhibited cell growth in concentration and pH-dependent manner. |
| Animal experiment [1, 2]: | |
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Animal models |
Mice bearing the LAGk-1A tumor, multiple myeloma xenograft(LAGk-2) mouse model |
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Dosage form |
Intravenous injection, 10.8 mg/kg; 3 times weekly at 1.8 mg/kg; once weekly at 5.4 mg/kg |
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Application |
In mice bearing the LAGk-1A tumor, INNO-206 (10.8 mg/kg, once weekly, i.v.) showed significantly smaller tumor volumes and IgG levels on days 28, 35 and 42. In LAGk-2–bearing mice, treatment with INNO-206 (i.v. 3 times weekly at 1.8 mg/kg) significantly reduced tumor volume. INNO-206 (once weekly, 5.4 mg/kg) showed significantly smaller tumor volumes. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. | |
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.
| Cas No. | 151038-96-9 | SDF | |
| 别名 | INNO-206;Doxorubicin-EMCH;INNO 206 | ||
| 化学名 | N-[(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 | ||
| Canonical SMILES | 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 | ||
| 分子式 | C37H42N4O13 | 分子量 | 750.75 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.332 mL | 6.66 mL | 13.32 mL |
| 5 mM | 0.2664 mL | 1.332 mL | 2.664 mL |
| 10 mM | 0.1332 mL | 0.666 mL | 1.332 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。