AVL-292 benzenesulfonate

Bruton's tyrosine kinase (Btk) plays a key role in promoting B cell proliferation and survival through participation in the BCR signaling pathway. AVL-292 is a highly selective small molecule inhibitor of Btk currently being evaluated in a Phase 1b clinical trial.
In vitro: AVL-292 forms a covalent bond with Cys481 in Btk and potently inhibits Btk in biochemical (IC50 < 0.5nM) and cellular assays (EC50 1-10 nM) including α-IgM stimulation of BCR signaling, B cell proliferation and activation [1].
In vivo: Oral efficacy of AVL-292 in an established CIA model in mice was measured. The dose-dependent inhibition of the clinical signs of inflammatory disease was observed during the in-life portion of the model. In addition, all three AVL-292dose levels prevented the loss in body weight typically associated with severity of disease observed in this model [2].
Clinical trial: In healthy human volunteers, AVL-292 was found to be safe and well tolerated following oral administration at dose levels ranging from 0.5 to 7.0 mg/kg. AVL-292 pharmacokinetic and pharmacodynamic measurement of Btk engagement was dose-proportional across cohorts [1].
Reference:
[1] 53rd ASH Annual Meeting and Exposition. Abstract 3485: Clinical Development of AVL-292; A Potent, Selective Covalent Btk Inhibitor for the Treatment of B Cell Malignancies.
[2] Evans EK, Tester R, Aslanian S, Karp R, Sheets M, Labenski MT, Witowski SR, Lounsbury H, Chaturvedi P, Mazdiyasni H, Zhu Z, Nacht M, Freed MI, Petter RC, Dubrovskiy A, Singh J, Westlin WF. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J Pharmacol Exp Ther. 2013;346(2):219-28.

A one-dimensional chloride-bridged Pt(II)/Pt(IV) mixed-valence complex with a 4-[(4-hydroxyphenyl)diazenyl]benzenesulfonate counter-ion.[Pubmed:26632826]

Acta Crystallogr C Struct Chem. 2015 Dec 1;71(Pt 12):1033-6.

The title compound, catena-poly[[[bis(ethylenediamine-kappa(2)N,N')platinum(II)]- mu-chlorido-[bis(ethylenediamine)platinum(IV)]-mu-chlorido] tetrakis{4-[(4-hydroxyphenyl)diazenyl]benzenesulfonate} dihydrate], {[Pt(II)Pt(IV)Cl2(C2H8N2)4](HOC6H4N=NC6H4SO3)4.2H2O}n, has a linear chain structure composed of square-planar [Pt(en)2](2+) (en is ethylenediamine) and elongated octahedral trans-[PtCl2(en)2](2+) cations stacked alternately, bridged by Cl atoms, along the b axis. The Pt atoms are located on an inversion centre, while the Cl atoms are disordered over two sites and form a zigzag ...Cl-Pt(IV)-Cl...Pt(II)... chain, with a Pt(IV)-Cl bond length of 2.3140 (14) A, an interatomic Pt(II)...Cl distance of 3.5969 (15) A and a Pt(IV)-Cl...Pt(II) angle of 170.66 (6) degrees . The structural parameter indicating the mixed-valence state of the Pt atom, expressed by delta = (Pt(IV)-Cl)/(Pt(II)...Cl), is 0.643.

Study of ciprofloxacin adsorption and regeneration of activated carbon prepared from Enteromorpha prolifera impregnated with H3PO4 and sodium benzenesulfonate.[Pubmed:28109901]

Ecotoxicol Environ Saf. 2017 May;139:36-42.

Activated carbons were derived from Enteromorpha prolifera immersed in H3PO4 solution or the H3PO4 solution mixed with sodium benzenesulfonate (SBS), producing AC and AC-SBS. NaOH solution was employed in regeneration of ciprofloxacin (CIP)-loaded AC and AC-SBS to obtain RAC and RAC-SBS. The properties of the original and regenerated activated carbons were characterized by thermo-gravimetric analysis (TGA), scanning electron microscopy (SEM), N2 adsorption/desorption isotherms and Fourier transform infrared spectroscopy (FTIR). Batched adsorption studies were carried out to compare CIP adsorption behaviors of the four carbons. The results suggested that the four samples exhibited higher proportions of mesopores and similar functional groups. Although AC displayed much higher specific surface area (SBET) (1045.79m(2)/g) than AC-SBS (738.03m(2)/g), its CIP adsorption capacity was much less than AC-SBS. The maximum adsorption capacity for AC, AC-SBS, RAC and RAC-SBS were found to be 250mg/g, 286mg/g, 233mg/g and 256mg/g, respectively, with the isotherms adhering to Langmuir isotherm model. The electrostatic attraction and cation exchange between CIP and the four carbons were the dominant adsorption mechanisms. Moreover, the thermodynamic parameters represented that the adsorption process had been confirmed to be a spontaneous and endothermic reaction.

Sulfonate salts of the therapeutic agent dapsone: 4-[(4-aminophenyl)sulfonyl]anilinium benzenesulfonate monohydrate and 4-[(4-aminophenyl)sulfonyl]anilinium methanesulfonate monohydrate.[Pubmed:27045177]

Acta Crystallogr C Struct Chem. 2016 Apr;72(Pt 4):280-4.

Dapsone, formerly used to treat leprosy, now has wider therapeutic applications. As is the case for many therapeutic agents, low aqueous solubility and high toxicity are the main problems associated with its use. Derivatization of its amino groups has been widely explored but shows no significant therapeutic improvements. Cocrystals have been prepared to understand not only its structural properties, but also its solubility and dissolution rate. Few salts of dapsone have been described. The title salts, C12H13N2O2S(+).C6H5O3S(-).H2O and C12H13N2O2S(+).CH3SO3(-).H2O, crystallize as hydrates and both compounds exhibit the same space group (monoclinic, P21/n). The asymmetric unit of each salt consists of a 4-[(4-aminophenyl)sulfonyl]anilinium monocation, the corresponding sulfonate anion and a water molecule. The cation, anion and water molecule form hydrogen-bonded networks through N-H...O=S, N-H...Owater and Owater-H...O=S hydrogen bonds. For both salts, the water molecules interact with one sulfonate anion and two anilinium cations. The benzenesulfonate salt forms a two-dimensional network, while the hydrogen bonding within the methanesulfonate salt results in a three-dimensional network.

Carbon dots as fluorescent probe for "off-on" Detecting sodium dodecyl-benzenesulfonate in aqueous solution.[Pubmed:26318701]

Spectrochim Acta A Mol Biomol Spectrosc. 2016 Jan 15;153:268-72.

In this paper, we propose an "off-on" approach for the detection of sodium dodecyl-benzenesulfonate (SDBS) using carbon dots (CDs) as fluorescent probe. We firstly demonstrated that the fluorescence of CDs decreased apparently in the presence of ruthenium (Ru), and the system was thus "turn-off". The resulting CDs-Ru system was found to be sensitive to SDBS, SDBS not only serves to shelter the CDs effectively from being quenched, but also to reverse the quenching and restore the fluorescence due to its ability to remove Ru from the surface of CDs (turn-on). An eco-friendly, simple and sensitive platform for the detection of SDBS based on the CDs-Ru probes has been proposed. After the experimental conditions were optimized, the linear range for detection SDBS was 0.10-7.50 mug/mL, with correlation coefficient (r) 0.9988, detection limit was 0.033 mug/mL (3sigma). This method is facile, rapid, low cost, environment-friendly, and possesses the potential for practical application.

Spebrutinib besylate (AVL-292 benzenesulfonate; CC-292 besylate) is a potent inhibitor of Btk kinase activity (IC50<0.5 nM, Kinact/Ki=7.69×104 M-1s-1s) in biochemical assays.

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