S65487 (Synonyms: VOB560) |
| カタログ番号GC62554 |
強力で選択的な BCL-2 阻害剤である S65487 (VOB560) は、S55746 のプロドラッグです。 S65487 は、G101V や D103Y などの BCL-2 変異に対しても活性があります。 S65487 は、MCL-1、BFL-1、BCL-XL との親和性が低くなります。 S65487 はアポトーシスを誘導し、抗がん作用があります。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1644600-79-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
S65487 (VOB560) is a potent and selective Bcl-2 inhibitor. S65487 is also active on BCL-2 mutations, such as G101V and D103Y. S65487 has poor affinity with MCL-1, BFL-1 and BCL-XL. S65487 induces apoptosis and has anticaner activities[1][2].
S65487 binds to the BH3 hydrophobic groove of BCL-2. S65487 induces apoptosis in a panel of hematological cancer cell lines and inhibits cell proliferation with IC50s in the low nM range[1].
S65487 induces complete regression in BCL-2-dependent RS4;11 tumors in vivo after a single IV (intravenous) administration. Strong and persistent tumor regression in xenograft models of lymphoid malignancies in mouse and rat are observed at well tolerated doses following weekly IV administration of S65487 in combination with the MCL-1-specific inhibitor, S64315/MIK665[1].
[1]. Arnaud Le Tiran, et al. Abstract 1276: Identification of S65487/VOB560 as a potent and selective intravenous 2nd-generation BCL-2 inhibitor active in wild-type and clinical mutants resistant to Venetoclax. Cancer Research. July 2021.
[2]. American Association for Cancer Research, AACR. 2021.4.10-15.
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *