点击图片查看原图
Technical Data:
M.Wt: 974.61
Formula: C47H55ClF3N5O6S3
Solubility: Unknown
Purity: 99%
Storage: at -20℃ 2 years
CAS No: 923564-51-6
Biological Activity:
A potent, orally bioavailable Bad-like BH3 mimetic (Ki's of <1 nmol/L for Bcl-2, Bcl-xL, and Bcl-w).ABT-263 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.
References:
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.
3, ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo. Ackler S, et al,Mol Cancer Ther. 2008 Oct;7(10):3265-74.