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EDO-S101

Cat. No. M6070
EDO-S101 Structure
Synonym:

Tinostamustine; EDO-S-101; EDO-S 101

Size Price Availability Quantity
5mg USD 280 In stock
10mg USD 580 In stock
25mg USD 1000 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: EDOS101 inhibits HDAC activity in rat peripheral blood mononuclear cells (PBMCs) in a cellular assay by approximately 90% one hour after dosing with 10mg/kg i.v. HDAC inhibition in PBMCs could not be increased with higher doses up to 50mg/kg. EDO-S101 triggers apoptosis and shows strong antitumor activity in HL60 and Daudi cells. Initial in vitro experiments in HL60 cells shows an activation of the intrinsic pathway of apoptosis with cleavage of caspases 3, 9 and PARP and a marked reduction of anti-apoptotic proteins XIAP and Mcl-1. In vivo: Intracellular HDAC inhibition of EDO-S101, which occurs rapidly after dosing is at maximum activity already at the lowest dose of 10mg/kg and lasts for about 12-16 hours. Exposure to EDO-S101 causes a strong DNA repair response evidenced by activation of pH2AX and p53 in tumors taken from mice bearing subcutaneous human Burkitt’s lymphoma. Tumors of BL rapidly shrink or are completely eradicated after i.v. administration of EDO-S101.

Protocol
Cell Experiment
Cell lines human MM cell lines
Preparation method MM1S cells were incubated for 48 h with increasing doses of EDO-S101, together with IL-6 at 1 nM or IGF-1 at 10 nM, and proliferation of MM cells was assessed by MTT assay.
Concentrations
Incubation time 48 h
Animal Experiment
Animal models Mice
Formulation
Dosages 60 mg/kg
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 415.36
Formula C19H28Cl2N4O2
CAS Number 1236199-60-2
Purity >99%
Solubility 30 mg/mL in DMSO
Storage at -20°C
References

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.
López-Iglesias AA, et al. J Hematol Oncol. 2017 Jun 20;;10(1):127. PMID: 28633670.

The Alkylating-HDAC Inhibition Fusion Principle: Taking Chemotherapy to the Next Level with the First in Class Molecule EDO-S101.
Mehrling T, et al. Anticancer Agents Med Chem. 2016;16(1):20-8. PMID: 25980817.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: EDO-S101, Tinostamustine; EDO-S-101; EDO-S 101 supplier, HDAC, inhibitors

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