DC Chemicals · Product datasheet

ASTX660(Tolinapant） — Datasheet

CAT. NO. DC20695

Product page and current package options

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.

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