Pyridoclax

Pyridoclax, also known as MR29072, is a potent and selective Mcl-1 inhibitor. Without cytotoxic activity when administered as a single agent, pyridoclax induced apoptosis in combination with Bcl-xL-targeting siRNA or with ABT-737 in ovarian, lung, and mesothelioma cancer cells. Bcl-xL and Mcl-1 cooperate to protect cancer cells against apoptosis and their concomitant inhibition leads to massive apoptosis even in the absence of chemotherapy. Whereas Bcl-xL inhibitors are now available, Mcl-1 inhibition, required to sensitize cells to Bcl-xL-targeting strategies, remains problematic.

Product information

CAS Number: 1651890-44-6

Molecular Weight: 426.51

Formula: C29H22N4

Synonym:

MR-29072

Chemical Name: 3-methyl-5-{5-[(E)-2-phenylethenyl]-[3,3'-bipyridin]-6-yl}-2,3'-bipyridine

Smiles: CC1=CC(=CN=C1C1=CN=CC=C1)C1=NC=C(C=C1/C=C/C1C=CC=CC=1)C1=CN=CC=C1

InChiKey: WGGSYXQFYRWBEC-VAWYXSNFSA-N

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+

Technical Data

Appearance: Solid Power

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

Solubility: Soluble in DMSO

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. Gloaguen C, Voisin-Chiret AS, Sopkova-de Oliveira Santos J, Fogha J, Gautier F, De Giorgi M, Burzicki G, Perato S, Pétigny-Lechartier C, Simonin-Le Jeune K, Brotin E, Goux D, N'Diaye M, Lambert B, Louis MH, Ligat L, Lopez F, Juin P, Bureau R, Rault S, Poulain L. First Evidence That Oligopyridines, α-Helix Foldamers, Inhibit Mcl-1 and Sensitize Ovarian Carcinoma Cells to Bcl-xL-Targeting Strategies. J Med Chem. 2015 Feb 26;58(4):1644-68.

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