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EDO-S101

Catalog No. T3516 CAS 1236199-60-2

Synonyms: Tinostamustine, Minomustine

EDO-S101 (Tinostamustine) is a pan HDAC inhibitor with IC50 values of 9, 9 and 25 nM for HDAC1, HDAC2 and HDAC3 , respectively.

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EDO-S101, CAS 1236199-60-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 43.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 77.00
10 mg	In stock	$ 126.00
25 mg	In stock	$ 207.00
50 mg	In stock	$ 369.00
1 mL * 10 mM (in DMSO)	In stock	$ 70.00

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Purity: 98.61%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	EDO-S101 (Tinostamustine) is a pan HDAC inhibitor with IC50 values of 9, 9 and 25 nM for HDAC1, HDAC2 and HDAC3 , respectively.
Targets&IC50	HDAC1:9nM, HDAC3:25 nM, HDAC2:9nM
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 10 mg/kg i.v. HDAC inhibition in PBMCs could not be increased with higher doses up to 50 mg/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 10 mg/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.
Kinase Assay	EDO-S101 is dissolved in DMSO and added to the assay buffer solution. EDO-S101 dilutions of 5 μL of each dilution is added to 50 μL of the reaction mixture including the Fluor de Lys substrate and all of the enzymatic reactions are conducted in duplicate at 37oC for 30 minutes. After enzymatic reactions, 50 μL of 2xHDAC developer is added to each well and fluorescence intensity is measured[1].

Synonyms	Tinostamustine, Minomustine
Molecular Weight	415.36
Formula	C19H28Cl2N4O2
CAS No.	1236199-60-2

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

HIF-1 Signaling Pathway Compound Library Cancer Cell Differentiation Compound Library Anti-Pancreatic Cancer Compound Library Anti-Breast Cancer Compound Library ReFRAME Related Library Reprogramming Compound Library Histone Modification Compound Library DNA Damage & Repair Compound Library Epigenetics Compound Library Target-Focused Phenotypic Screening Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

EDO-S101 1236199-60-2 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Histone deacetylases Inhibitor Tinostamustine EDOS101 inhibit EDO S101 Minomustine EDO-S-101 EDO-S 101 inhibitor

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