[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

MDLMFCD31619274
Molecular Weight539.68
Molecular FormulaC30H42FN5O3
SMILESC[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

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.8529 mL9.2647 mL18.5295 mL
5 mM0.3706 mL1.8529 mL3.7059 mL
10 mM0.1853 mL0.9265 mL1.8529 mL
50 mM0.0371 mL0.1853 mL0.3706 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.

Targets

cIAP2 [1]cIAP1 [1]
(Cell-free assay)
XIAP [1]
(Cell-free assay)
12 nM40 nM

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.