Supinoxin 是磷酸化 p68 RNA 解旋酶的强效口服活性抑制剂，是一种抗肿瘤试剂。它与 Y593 磷酸化的 p68 相互作用并减弱 β-CATenin 的核穿梭性。它诱导细胞凋亡并抑制 TNBC 癌细胞系的生长，IC50的范围为 10 nM 至 20 nM。

Supinoxin is an orally active inhibitor of phosphorylated-p68 RNA helicase and a potent first-in-class anti-cancer agent. Supinoxin induces cell apoptosis and inhibits the growth of TNBC cancer cell lines (IC50s:10 nM - 20 nM).

Supinoxin inhibits cell growth, MDA-MB-231, Caki-1, UMRC2, PANC-1, A549, MKN-45, HepG2, HCT116, HT29, PC-3, U251, HeLa, SK-MEL-28 and OVCAR-3 (IC50: range from 0.01 μM to 0.021 μM in the growth inhibition of cancer cells). Supinoxin (0-10 μM; 72 hours) is active against cell lines of all TNBC molecular subtypes and is active against cell lines with mutations in p53, RB1, CDKN2A, and loss of PTEN. Supinoxin (20-100 nM; 24 hours) treatment causes a dose-dependent increase in tetraploid cells, consistent with induction of G2–M cell-cycle arrest. Supinoxin (0-100 nM; 24 or 48 hours) reduces MCL-1 expression in a dose-dependent manner in TNBC cell lines sensitive to Supinoxin. Supinoxin (0-100 nM; 72 hours) exhibits no significant induction of apoptosis in cell lines resistant to the antiproliferative effects of Supinoxin. But in sensitive cells, the observed activation of apoptosis begins at 24–48 hours and reaches a peak at 72 hours. The induced apoptosis is treated with a dose of 100 nM [1][2].

Supinoxin (p.o.; 160/320/600 mg/kg; once weekly for 3 weeks) obviously dose-dependent tumor growth inhibition in the MDA-MB-231 model, exhibits TGI of 55.7%, 80.29% and 94.58% at 160 mg/kg, 320 mg/kg and 600 mg/kg, respectively [1].

888478-45-3

C22H24FN5O4

441.46

RX-5902

DMSO:100 mg/mL (226.52 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years