ASTX660(Tolinapant) chemical structure
Chemical structureResearch use only
CAT. NO. DC20695Featured

ASTX660(Tolinapant)

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TotalUS$850
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Product overview

Description & Application

ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).

ParameterValue
Chemical Name1-(6-(4-fluorobenzyl)-5-(hydroxymethyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)-2-((2R,5R)-5-methyl-2-(((R)-3-methylmorpholino)methyl)piperazin-1-yl)ethan-1-one
CAS No.1799328-86-1
SynonymsASTX 660;ASTX-660
FormulaC30H42FN5O3
M.Wt539.684590816498
SMILESC[C@@H]1COCCN1C[C@H]1CN[C@H](C)CN1CC(=O)N1C2C(=NC(=C(C=2)CC2C=CC(F)=CC=2)CO)C(C)(C)C1
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).

In Vitro

ASTX660 is an orally bioavailable dual antagonist of cIAP and XIAP, currently being investigated in a single-agent Phase 1/2 clinical trial in patients with advanced solid tumors and lymphomas. Twenty-one triple-negative breast cancer (TNBC) cell lines are treated with ASTX660 in vitro and it is found that 43% are sensitive to ASTX660[1].

In Vivo

In HCC1806 xenografts in mice, ASTX660 (daily oral treatment) causes moderate tumor growth inhibition but not regression[1].

References & source

[1]. Tomoko Smyth, et al. Abstract 1287: The dual IAP antagonist, ASTX660, increases the anti-tumor activity of NSC 125973 in preclinical models of triple-negative breast cancer in vivo. Cancer Res 2016;76(14 Suppl).

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

Refer to the certificate supplied with your lot for batch-specific release results.

Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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