2015年12月3日 · SL-801 is a novel small molecule that binds covalently to Cys528 of XPO1, blocking the ability of XPO1 to interact with substrate cargos (e.g., p53, FOXO, p21, p27, and others).

2015年12月3日 · SL-801 is a novel small molecule that binds covalently to Cys528 of XPO1, blocking the ability of XPO1 to interact with substrate cargos (e.g., p53, FOXO, p21, p27, and others).

- SL-801 was cytotoxic towards solid and hematologic cancer cell lines regardless of mutation status of key oncogenes and tumor suppressor genes. • The anti-tumor effects of SL-801 were validated in vivo in several SCID xenograft models. - SL-801 significantly extended overall survival in the ARH-77 and

Study SL-801-0115 is a dose-escalation study evaluating multiple doses and schedules of orally administered SL-801 in participants with advanced solid tumors. Targeting XPO1 inhibition has emerged as a promising therapeutic strategy in cancer treatment. Despite the numerous XPO1 inhibitors reported to date, no XPO1 degraders have been disclosed.

SL-801 is a novel, oral, small-molecule reversible inhibitor of exportin-1 (XPO1), a key nuclear transport protein. XPO1 is overexpressed by many cancers, leading to mislocalization of key tumor suppressors and growth-regulatory proteins in the cytoplasm. A Phase 1 trial is ongoing, and currently enrolling patients with advanced solid tumors.

SL-801 has demonstrated potent in vitro and in vivo anti-tumor activity against a broad range of hematologic and solid cancers. SL-801’s reversible inhibition of XPO-1 may translate to selective activity and potential safety benefits. Interim results from the dose-escalation study are reported.

Felezonexor（CBS9106；SL-801）是一种新型的可逆的口服CRM1抑制剂，具有CRM1降解活性而不影响CRM1 mRNA水平。 Felezonexor也是一种可逆的XPO1抑制剂，通过与Cys528共价结合以及诱导XPO1的降解来抑制核出口。

2019年10月1日 · SL-801 is a novel, oral, small molecule that reversibly inhibits Exportin-1 (XPO-1), a nuclear export protein, overexpressed in a variety of solid and hematologic malignancies. XPO-1 is a mediator of nuclear-cytoplasmic transport of over 200 nuclear proteins and has been associated with aggressive tumor behavior and poor prognosis.

2015年5月20日 · SL-801 is a structurally novel small molecule that binds covalently but reversibly to XPO1, blocking binding of substrate cargos. The kinetics of target binding and preclinical activity of SL-801 in multiple tumor types are reported here.

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