Pyridoclax

• CAT Number: I002160
• CAS Number: 1651890-44-6
• Molecular Formula: C₂₉H₂₂N₄
• Molecular Weight: 426.51
• Purity: ≥95%
• Target: Bcl-2 Family
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 25 nM(Kd) [1]
• InChI: InChI=1S/C29H22N4/c1-21-15-27(20-32-28(21)25-10-6-14-31-18-25)29-23(12-11-22-7-3-2-4-8-22)16-26(19-33-29)24-9-5-13-30-17-24/h2-20H,1H3/b12-11+
• InChIKey: WGGSYXQFYRWBEC-VAWYXSNFSA-N
• SMILES: CC1=C(N=CC(=C1)C2=C(C=C(C=N2)C3=CN=CC=C3)C=CC4=CC=CC=C4)C5=CN=CC=C5

Pyridoclax (Cat.No:I002160) is a small molecule compound that acts as a selective inhibitor of B-cell lymphoma-2 (Bcl-2) proteins. It has shown potential as a novel anticancer agent by inducing apoptosis in cancer cells and disrupting Bcl-2-mediated anti-apoptotic pathways. Pyridoclax is currently being investigated in preclinical studies for its therapeutic applications in cancer treatment.

Reference

1:Eur J Pharm Sci. 2017 Jan 15;97:218-226. doi: 10.1016/j.ejps.2016.11.025. Epub 2016 Dec 1. Comparison of 2 strategies to enhance pyridoclax solubility: Nanoemulsion delivery system versus salt synthesis.Groo AC,De Pascale M,Voisin-Chiret AS,Corvaisier S,Since M,Malzert-Fréon A, PMID: 27916693 DOI: 10.1016/j.ejps.2016.11.025 Abstract: Pyridoclax is an original oligopyridine lead, very promising in treatment of chemoresistant cancers. However, from solubility measurement and permeability evaluation, it appeared that this compound can be considered as a BCS II drug, with a poor water solubility. To overcome this unfavorable property, two strategies were proposed and compared: pyridoclax di-hydrochloride salt synthesis and formulation of pyridoclax-loaded nanoemulsions (PNEs) efficiently performed by transposing the spontaneous emulsification process previously developed by our team. Whereas the salt improved the thermodynamic solubility of the drug by a factor 4, the apparent solubility of the encapsulated pyridoclax was 1000-fold higher. Their stability was assessed upon dilution in various complex biomimetic media relevant for oral administration (SGF, FaSSIF-V2, FeSSIF-V2) or for the intravenous route (PBS). The solubility of the salt was affected by the nature of the medium, indicating that it could precipitate after administration, negatively impacting its bioavailability and its efficiency in vivo. On the contrary, in all media, PNEs remained stable in terms of granulometric properties (determined by DLS), ζ-potential and encapsulation efficiency (measured by HPLC). Thus, such nanomedicines appear as a valuable option to perform preclinical studies on the promising pyridoclax.Copyright © 2016 Elsevier B.V. All rights reserved.