RGNCY-0125 (S-40 Tubulin inhibitor a)

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S-40 is a novel, orally potent tubulin destabilisation compound.  Data from crystal structure analysis revealed that S-40 occupies all three zones in the colchicine pocket with interactions distinct from other known microtubule inhibitors.  S-40 overcomes paclitaxel-resistance and lacks neurotoxicity which are the limiting factors in the clinical use of paclitaxel in the treatment of cancer.  S-40 inhibits the growth of cancer cell lines and patient derived organoids by inducing mitotic arrest and apoptosis.  Daily oral administration of S-40 in xenograft mouse models significantly inhibited growth of non- small cell lung cancer NCI-H1299, human prostate cancer DU145 and pacltaxel-resistant A549 without apparent side effects.  S-40 represents a new generation of orally effective microtubule inhibitors for cancer therapy.  

Systematic Name: 3-((4-cyclopropylphenyl)sulfonamido)-4-methyl-N-(pyridin-3-ylmethyl)benzamide

SMILES:  O=C(C1=CC=C(C)C(NS(C2=CC=C(C3CC3)C=C2)(=O)=O)=C1)NCC4=CN=CC=C4

Formula:  C23H23N3O3S

Mol Wt: 421.52