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- 文献和实验
- 技术资料
- 保存条件:
Powder:-20℃,2 years
- 保质期:
Powder:-20℃,2 years
- 英文名:
Aldoxorubicin
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
1361644-26-9
- 规格:
10mg/5mg/2mg
| 规格: | 10mg | 产品价格: | ¥1730.0 |
|---|---|---|---|
| 规格: | 5mg | 产品价格: | ¥1190.0 |
| 规格: | 2mg | 产品价格: | ¥740.0 |
| 基本信息 | |
| CAS | No.1361644-26-9 |
| 英文名称 | Aldoxorubicin |
| 别名 | INNO-206;ALDOXORUBICIN;CS-1186;Aldoxorubicin(USAN);DOXO-EMCH; |
| 分子式 | C37H42N4O13 |
| 分子量 | 750.75 |
| 溶解性 | Soluble in DMSO ≥5mg/mL(Need ultrasonic)(该产品在溶液状态不稳定,建议您现用现配) |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:-20℃,2 years |
| MDL | MFCD15146982 |
| SMILES | C[C@H]1[C@H]([C@H](C[C@@H](O1)O[C@H]2C[C@@](CC3=C2C(=C4C(=C3O)C(=O)C5=C(C4=O)C(=CC=C5)OC)O)(/C(=N/NC(=O)CCCCCN6C(=O)C=CC6=O)/CO)O)N)O |
| InChIKey | OBMJQRLIQQTJLR-USGQOSEYSA-N |
| InChI | InChI=1S/C37H42N4O13/c1-17-32(46)20(38)13-27(53-17)54-22-15-37(51,23(16-42)39-40-24(43)9-4-3-5-12-41-25(44)10-11-26(41)45)14-19-29(22)36(50)31-30(34(19)48)33(47)18-7-6-8-21(52-2)28(18)35(31)49/h6-8,10-11,17,20,22,27,32,42,46,48,50-51H,3-5,9,12-16,38H2,1-2H3,(H,40,43)/b39-23+/t17-,20-,22-,27-,32+,37-/m0/s1 |
| PubChem CID | 9810709 |
| 靶点 | Others |
| 通路 | Others |
| 背景说明 | 是一种化合物,具有抗肿瘤活性。 |
| 生物活性 | 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.[1-4] |
| 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[1]. |
| 细胞实验 | 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[1]. Aldoxorubicin (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]. Aldoxorubicin (INNO-206) shows superior activity over doxorubicin in a murine renal cell carcinoma model and in breast carcinoma xenograft models[3]. |
| 细胞实验 | Cells are seeded at 1×105?cells/100 μL/well in 96-well plates in RPMI-1640 media with FBS for 24 hours before treatment. Cells are cultured in the presence of medium, Aldoxorubicin (INNO-206) or doxorubicin for 48 hours. Next, cell viability is quantified using the CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay. Each well is treated with MTS for 1 to 4 hours, after which absorbance at 490 nm is recorded using a 96-well plate reader. The quantity of formazan product as measured is directly proportional to the number of living cells. Data graphed are means±SEM using 3 replicates per data point.[1-4] |
| 动物实验 | For the LAGκ-1A experiment, Aldoxorubicin (INNO-206) is administered to SCID mice at 10.8 mg/kg (doxorubicin equivalent dose of 8.0 mg/kg) once weekly. Mice are treated with conventional doxorubicin at 4.0 and 8.0 mg/kg once weekly. For the LAGκ-2 experiment, Aldoxorubicin (INNO-206) is administered once weekly (W) at doses of 2.7 and 5.4 mg/kg, or on 3 consecutive days (W-F) weekly at doses of 0.9 and 1.8 mg/kg. PS-341 is administered twice weekly (W, F) at a dose of 0.5 mg/kg. Doxorubicin is administered to SCID mice at 2, 4, and 8 mg/kg, and PLD is administered to SCID mice at 2 mg/kg once weekly. Each drug is administered i.v. in a volume of 100 μL.[1-4] |
| 数据来源文献 | [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 [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. |
| 单位 | 瓶 |
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