[CAS NO. 1799328-86-1] Tolinapant (ASTX660)
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PRODUCTS SPECIFICATIONS [1799328-86-1]
Catelog
SLK-S8681
Brand
Selleck
CAS
1799328-86-1
DESCRIPTION [1799328-86-1]
Overview
| MDL | MFCD31619274 |
|---|---|
| Molecular Weight | 539.68 |
| Molecular Formula | C30H42FN5O3 |
| SMILES | C[C@H]1N(C[C@@H]2N(CC(N3CC(C)(C)C4=NC(CO)=C(CC5=CC=C(F)C=C5)C=C43)=O)C[C@@H](C)NC2)CCOC1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
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.
In vitro
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.
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