An HDAC inhibitor and DNA alkylating agent
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

EDO-S101

Item No. 23328

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[bis(2-chloroethyl)amino]-N-hydroxy-1-methyl-1H-benzimidazole-2-heptanamide
CAS Number
1236199-60-2
Synonyms
  • Tinostamustine
Molecular Formula
C19H28Cl2N4O2
Formula Weight
415.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 5 mg/mlDMSO:PBS (pH 7.2)(1:9): 0.1 mg/ml
λmax
231, 324 nm
SMILES
CN1C2=CC=C(N(CCCl)CCCl)C=C2N=C1CCCCCCC(NO)=O
InChi Code
InChI=1S/C19H28Cl2N4O2/c1-24-17-9-8-15(25(12-10-20)13-11-21)14-16(17)22-18(24)6-4-2-3-5-7-19(26)23-27/h8-9,14,27H,2-7,10-13H2,1H3,(H,23,26)
InChi Key
GISXTRIGVCKQBX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $50

    Add

    5 mg

    $99

    Add

    10 mg

    $149

    Add
    Cayman Chemical
    Visit Our Cancer Resource Center
    Find Tools & Resources to Study the Hallmarks of Cancer
    • Cancer cell signaling & regulation
    • Cancer metabolism
    • Tumor microenvironment
    EXPLORE NOW
    Product Description

    EDO-S101 is a fusion molecule composed of the DNA alkylating agent bendamustine and the histone deacetylase (HDAC) inhibitor SAHA (Item No. 10009929) that inhibits class I and II HDACs (IC50s = 9-107 nM for HDAC1-3, 6, 8, and 10).1 It inhibits HDAC activity in rat peripheral blood mononuclear cells (PBMCs) ex vivo by 90% following a single dose of 10 mg/kg. EDO-S101 also induces formation of DNA crosslinks and double-strand breaks in HL-60 cells. It reduces growth of multiple myeloma (MM) cell lines irrespective of p53 mutational status or established resistance to DNA alkylating agents (IC50s = 1.6-4.8 μM).2 EDO-S101 also induces MM cell death ex vivo in bone marrow samples isolated from patients with early- and late-stage MM. In vivo, EDO-S101 (60 mg/kg per week) reduces tumor growth and prolongs survival in an MM1S end-stage mouse xenograft model. It also prolongs survival in a multidrug resistant Vk12653 mouse transplant model of refractory MM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mehrling, T., and Chen, Y. The alkylating-HDAC inhibition fusion principle: Taking chemotherapy to the next level with the first in class molecule EDO-S101. Anticancer Agents Med. Chem. 16(1), 20-28 (2016).

    2. López-Iglesias, A.A., Herrero, A.B., Chesi, M., et al. Preclinical anti-myeloma activity of EDO-S101, a new bendamustine-derived molecule with added HDACi activity, through potent DNA damage induction and impairment of DNA repair. J. Hematol. Oncol. 10(1), 127 (2017).