Arsthinol

Arsthinol is an antiprotozoal agent which may have anti-cancer activity. It was found that arsthinol, a trivalent organoarsenic compound (dithiarsolane), has been active in vitro on leukemia cell lines and offers a better therapeutic index than arsenic trioxide, as estimated by the ratio LD50/IC50. Arsthinol induced growth inhibition of NB4 cells at lower concentration (IC50 (concentration inhibiting growth by 50%) = 0.78 +/- 0.08 micromol/l after 24 h) than As(2)O(3) (IC50 = 1.60 +/- 0.23 micromol/l after 24 h) or melarsoprol (IC50 = 1.44 +/- 0.08 micromol/l after 24 h). Arsthinol-cyclodextrin complex demonstrated to have was more effective than arsenic trioxide (As2O3) and melarsoprol on the U87 MG cell line. Importantly, in the in vivo study, significant antitumor activity against heterotopic xenografts was observed after i.p. administration.

Product information

CAS Number: 119-96-0

Molecular Weight: 347.29

Formula: C11H14AsNO3S2

Chemical Name: N-(2-hydroxy-5-(4-(hydroxymethyl)-1, 3, 2-dithiarsolan-2-yl)phenyl)acetamide

Smiles: CC(=O)NC1=CC(=CC=C1O)[As]1SC(CS1)CO

InChiKey: MRUDSZSRLQAPOG-UHFFFAOYSA-N

InChi: InChI=1S/C11H14AsNO3S2/c1-7(15)13-10-4-8(2-3-11(10)16)12-17-6-9(5-14)18-12/h2-4,9,14,16H,5-6H2,1H3,(H,13,15)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Becherirat S, Lanhers MC, Socha M, Yemloul M, Astier A, Loboda C, Aniceto N, Gibaud S. The antitumor effects of an arsthinol-cyclodextrin complex in a heterotopic mouse model of glioma. Eur J Pharm Biopharm. 2013 Nov;85(3 Pt A):560-8. doi: 10.1016/j.ejpb.2013.06.021. Epub 2013 Jul 4. PMID: 23831266.
2. Ajana I, Astier A, Gibaud S. Speciation of arsenic in urine following intravenous administration of arsthinol in mice. Eur J Drug Metab Pharmacokinet. 2010 Sep;35(1-2):59-65. doi: 10.1007/s13318-010-0009-6. PMID: 21495268.
3. Ajana I, Astier A, Gibaud S. Arsthinol nanosuspensions: pharmacokinetics and anti-leukaemic activity on NB4 promyelocytic leukaemia cells. J Pharm Pharmacol. 2009 Oct;61(10):1295-301. doi: 10.1211/jpp/61.10.0004. PMID: 19814860.

Products are for research use only. Not for human use.