923564-51-6

Solubility:DMSO

Storage:at -20℃ 2 years

Biologieal

A potent, orally bioavailable Bad-like BH3 mimetic (Ki's of <1 nmol/L for Bcl-2, Bcl-xL, and Bcl-w).ABT-263(Navitoclax) disrupts Bcl-2/Bcl-xL interactions with prodeath proteins (e.g., Bim), leading to the initiation of apoptosis within 2 hours posttreatment. In human tumor cells, ABT-263 induces Bax translocation, cytochrome c release, and subsequent apoptosis. Oral administration of ABT-263 alone induces complete tumor regressions in xenograft models of small-cell lung cancer and acute lymphoblastic leukemia.

Navitoclax(ABT263) is a small molecule that is designed to restore apoptosis, also known as programmed cell death, by blocking the function of pro-survival Bcl-2 family proteins. Apoptosis is a natural process by which damaged or unwanted cells, including those that are cancerous, die and are cleared from the body. The Bcl-2 family proteins, which are expressed at high levels in many tumors, play a central role in regulating apoptosis and, consequently, are thought to impact tumor formation, tumor growth and resistance.

Reference

1, ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor.Tse C et al, Cancer Res. 2008 May 1;68(9):3421-8.

2, Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models. Shoemaker AR, et al. Clin Cancer Res. 2008 Jun 1;14(11):3268-77.