RGN6024

RGN6024 is a brain-penetrant, orally active and reversible small molecule tubulin destabilizer. RGN6024 inhibits microtubule polymerization both in biochemical and cellular assays, binds to the colchicine binding pocket of β-tubulin (SPR: Kd = 6.7 μM; tryptophan assay: Kd = 7.4 μM), and triggers G2/M arrest in glioblastoma (GB) cells. RGN6024 retains activity in βIII-tubulin overexpressing cells. RGN6024 inhibits tumor growth in a GB xenograft mouse model. RGN6024 can be used for the study of glioblastoma (GB) [1].

Product Specifications

CAS Number

[3055038-20-2]

UNSPSC

12352005

Target

Microtubule/Tubulin

Related Pathways

Cell Cycle/DNA Damage; Cytoskeleton

Field of Research

Cancer

Smiles

O=C(NC1=NC=C(OC2=CN=C(N=C2)N3CCOCC3)S1)C45CC(OC)(C5)C4

Molecular Formula

C18H21N5O4S

Molecular Weight

403.46

References & Citations

[1]Patrón LA, et al. RGN6024 Is a Brain-Penetrant, Small-Molecule Tubulin Destabilizer for the Treatment of Glioblastoma. Mol Cancer Ther. 2025 Aug 1;24 (8) :1129-1144. doi: 10.1158/1535-7163.MCT-24-1208