1. Cell Cycle/DNA Damage
    Antibody-drug Conjugate/ADC Related
  2. Topoisomerase
    ADC Cytotoxin
  3. Aldoxorubicin

Aldoxorubicin (Synonyms: INNO-206; DOXO-EMCH)

目录号: HY-16261 纯度: 95.58%
产品使用指南

Aldoxorubicin (INNO-206) 是多柔比星 (DNA 拓扑异构酶 II 抑制剂) 的白蛋白结合前药,在酸性条件下从白蛋白中释放出来。 Aldoxorubicin (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。

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Aldoxorubicin Chemical Structure

Aldoxorubicin Chemical Structure

CAS No. : 1361644-26-9

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Customer Review

Other Forms of Aldoxorubicin:

Top Publications Citing Use of Products

    Aldoxorubicin purchased from MCE. Usage Cited in: Br J Pharmacol. 2017 Sep;174(17):2862-2879.

    HSA decorated with Cy7 could be imaged. Through this strategy, the drug distribution of the HSA-decorated form and unbound form are imaged, and the merge rates are also calculated.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    Description

    Aldoxorubicin (INNO-206) is an albumin-binding prodrug 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.

    IC50 & Target[4]

    Topoisomerase II

     

    Daunorubicins/Doxorubicins

     

    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].

    In Vivo

    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].

    Clinical Trial
    Molecular Weight

    750.75

    Formula

    C₃₇H₄₂N₄O₁₃

    CAS No.

    1361644-26-9

    SMILES

    [H][C@@]1(O[C@H]2C[C@@](/C(CO)=N/NC(CCCCCN3C(C=CC3=O)=O)=O)(O)CC(C2=C4O)=C(O)C5=C4C(C6=C(OC)C=CC=C6C5=O)=O)O[C@@H](C)[C@@H](O)[C@@H](N)C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years

    *该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    Solvent & Solubility
    In Vitro: 

    DMSO : 75 mg/mL (99.90 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.3320 mL 6.6600 mL 13.3200 mL
    5 mM 0.2664 mL 1.3320 mL 2.6640 mL
    10 mM 0.1332 mL 0.6660 mL 1.3320 mL
    *

    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;该产品在溶液状态不稳定,建议您现用现配,即刻使用

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (3.33 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.33 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,澄清透明的生理盐水溶液
    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (3.33 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.33 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定溶至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (3.33 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.33 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    References
    Cell Assay
    [1]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    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. Bortezomib 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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    × = ×
    C1   V1   C2   V2

    Keywords:

    AldoxorubicinINNO-206DOXO-EMCHINNO206INNO 206TopoisomeraseADC CytotoxinInhibitorinhibitorinhibit

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