ST-401 

ST-401, a microtubule-targeting agent (MTA), is a brain-penetrant microtubule (MT) assembly inhibitor. ST-401 disrupts microtubule (MT) function through gentle and reverisible reduction in MT assembly that triggers mitotic delay and cell death in interphase. ST-401 shows a potent antitumor activity^[1].

ST-401 is a hybrid molecule that combines a secondary alcohol and quinoline in one structure. ST-401 competes for 89% of [3H]colchicine binding to tubulin. In a turbidity assay, ST-401 inhibits tubulin assembly with an IC₅₀ of 1.1 µM. In a pelleting assay that measures release of free tubulin, ST-401 inhibits tubulin assembly with comparable IC₅₀ value of 3.2 µM^[1].
ST-401 exhibits similar antitumor activities in the low nanomolar range in most human cancer cell lines, including the six glioma lines (SF-268, SF-295, SF-539, SNB-19, SNB-75, and U251: IC50s 23-69 nM)^[1].
ST-401 shows the antitumor activity in PD-glioma is in the low nanomolar (IC50: 24-47 nM)^[1].
ST-401 (72 h) reduces overall cell viability in MGG8 and T98G cells with comparable IC₅₀s (14 and 36 nM, respectively)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ST-401 (20 mg/kg; i.p; bidaily; 5 days/week for 4 weeks) demonstrates significant antitumor activity and no over toxicity in a xenograft flank tumor mouse model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

352.43

C₂₄H₂₀N₂O

2419942-78-0

Solid

White to light yellow

OC(C1=CC=CC2=C1C=CC=N2)C3=CC4=C(C=C3)N(CC)C5=CC=CC=C54

Room temperature in continental US; may vary elsewhere.

• [1]. Eric A Horne, et al. A brain-penetrant microtubule-targeting agent that disrupts hallmarks of glioma tumorigenesis. Neurooncol Adv. 2020 Dec 3;3(1):vdaa165.  [Content Brief]