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

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

Cat. No.: HY-16261 Purity: >95.0%
Data Sheet SDS Handling Instructions

INNO-206 is a prodrug of the anticancer agent doxorubicin, which is released from albumin under acidic conditions.

For research use only. We do not sell to patients.
INNO-206 Chemical Structure

INNO-206 Chemical Structure

CAS No. : 1361644-26-9

Size Price Stock Quantity
5 mg $135 In-stock
10 mg $174 In-stock
50 mg $595 In-stock
100 mg $873 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of INNO-206:

    INNO-206 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.

    INNO-206 purchased from MCE. Usage Cited in: ACS Med Chem Lett. 2015 Jun 22;6(8):948-52.

    Combination treatment. (a) Comparison of AZD-8055 and ABT-263 treatment in all cell lines. Red indicates sensitivity, while blue indicates resistance. (b) Depiction of synergism where the values shown are excess over Bliss Independence, a prediction of inhibition without synergism. Increased synergism is evident by an increased number, shown in red, while negative numbers in blue represent an antagonistic effect.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    INNO-206 is a prodrug of the anticancer agent doxorubicin, which is released from albumin under acidic conditions.

    In Vitro

    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

    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]. 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]. INNO-206 shows superior activity over doxorubicin in a murine renal cell carcinoma model and in breast carcinoma xenograft models[3].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT01706835 CytRx Advanced Solid Tumors October 2012 Phase 1
    NCT01673438 CytRx Advanced Solid Tumor July 2012 Phase 1
    NCT02014844 CytRx Glioblastoma March 2014 Phase 2
    NCT02029430 CytRx Kaposi's Sarcoma|HIV+|HIV Positive|AIDS January 2014 Phase 2
    NCT02235688 CytRx Metastatic Solid Tumors August 2014 Phase 1
    NCT02235701 CytRx Metastatic, Locally Advanced, or Unresectable Soft Tissue Sarcoma August 2014 Phase 1|Phase 2
    NCT02200757 CytRx Metastatic Small Cell Lung Cancer September 2014 Phase 2
    NCT02570412 CytRx Sarcoma
    NCT02049905 CytRx Metastatic, Locally Advanced or Unresectable Soft Tissue Sarcoma January 2014 Phase 3
    NCT01706835 CytRx Advanced Solid Tumors October 2012 Phase 1
    NCT01673438 CytRx Advanced Solid Tumor July 2012 Phase 1
    NCT02014844 CytRx Glioblastoma March 2014 Phase 2
    NCT02029430 CytRx Kaposi's Sarcoma|HIV+|HIV Positive|AIDS January 2014 Phase 2
    NCT02235688 CytRx Metastatic Solid Tumors August 2014 Phase 1
    NCT02235701 CytRx Metastatic, Locally Advanced, or Unresectable Soft Tissue Sarcoma August 2014 Phase 1|Phase 2
    NCT02200757 CytRx Metastatic Small Cell Lung Cancer September 2014 Phase 2
    NCT02570412 CytRx Sarcoma
    NCT02049905 CytRx Metastatic, Locally Advanced or Unresectable Soft Tissue Sarcoma January 2014 Phase 3
    NCT01337505 CytRx Malignant Solid Tumour April 2011 Phase 1
    NCT01580397 CytRx Pancreatic Ductal Adenocarcinoma May 2012 Phase 2
    NCT01514188 CytRx Metastatic Soft Tissue Sarcoma|Locally Advanced Soft Tissue Sarcoma|Unresectable Soft Tissue Sarcoma December 2011 Phase 2
    NCT00472771 CytRx Small Cell Lung Cancer May 2008 Phase 2
    View MoreCollapse
    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) 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
    Cell Assay
    [1]

    INNO-206 stock solutions (5.4 mg/mL) are prepared using 50% ethanol and 50% water and further diluted in sterile water.

    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, 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, 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, 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
    Molecular Weight

    750.75

    Formula

    C₃₇H₄₂N₄O₁₃

    CAS No.

    1361644-26-9

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: >95.0%

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    Inquiry Information

    Product Name:
    INNO-206
    Cat. No.:
    HY-16261
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