Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
1.8529 mL
9.2647 mL
18.5295 mL
5 mM
0.3706 mL
1.8529 mL
3.7059 mL
10 mM
0.1853 mL
0.9265 mL
1.8529 mL
50 mM
0.0371 mL
0.1853 mL
0.3706 mL
Description
Tolinapant (ASTX660) is a potent, non-peptidomimetic antagonist of and that inhibits the interactions between a SMAC-derived peptide and the BIR3 domains of XIAP (BIR3-XIAP) and cIAP1 (BIR3-cIAP1) with IC50 values less than 40 and 12 nmol/L, respectively.
ASTX660 induces proteasomal degradation of cIAP1 and 2, resulting in downstream effects of NIK stabilization and activation of noncanonical NF-kB signaling, demonstrating cIAP1/2 antagonism. Because of their roles in the evasion of apoptosis, inhibitor of apoptosis proteins (IAP) are considered attractive targets for anticancer therapy. Treatment with ASTX660 leads to TNFa-dependent induction of apoptosis in various cancer cell lines in vitro.
