RSL-3

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种致癌 RAS 选择性致死化合物，可激活携带致癌 RAS 的癌细胞中铁依赖性、非凋亡性细胞死亡。

An oncogenic RAS-selective lethal compound that actvates iron-dependent, nonapoptotic cell death in oncogenic-RAS-harboring cancer cells, inhibits glutathione peroxidase (GPX4) and induces ferroptosis in BJeLR cells (EC50=10 nM); increases PTGS2 expression and significantly inhibits tumor growth in a xenograft mouse model (100 mg/kg).(In Vitro):RSL3 (0-8 μM, 72 hours) potently reduces the viability of HN3 cells, with IC50s of 0.48 μM in HN3 and 5.8 μM in HN3-rslR cells, respectively.RSL3 (0-8 μM, 24 hours) reduces the expression of GPX4 protein, increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells.(In Vivo):RSL3 (100 mg/kg, Intratumorally twice per week for 20 days) significantly inhibits the growth of tumor in combination with trigonelline in mice bearing HN3R cells.

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Animal Model:Ten-week-old athymic BALB/c male nude mice (nu/nu) bearing HN3R cells Dosage:100 mg/kg in combination with trigonelline (50 mg/kg) Administration:Intratumorally twice per week for 20 days Result:Significantly reduced the volume of tumor combined with trigonelline in mice.

RSL3 | 1S,3R-RSL3

Apoptosis

Ferroptosis

Ferroptosis

Cancer

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1219810-16-8

440.8763

C23H21ClN2O5

>98% (HPLC)

DMSO: ≥ 31 mg/mL

O=C(OC)[C@@H]1N(C(CCl)=O)[C@@H](C2=CC=C(C(OC)=O)C=C2)C3=C(C(C=CC=C4)=C4N3)C1

1H-Pyrido[3,4-b]indole-3-carboxylic acid, 2-(2-chloroacetyl)-2,3,4,9-tetrahydro-1-[4-(methoxycarbonyl)phenyl]-, methyl ester, (1S,3R)-

(-20℃)

With Ice Pack

≥ 2 years