1799328-86-1

1799328-86-1 structure

Name: ASTX660
Chemical Name: ASTX660
CAS Number: 1799328-86-1
Molecular Formula: C₃₀H₄₂FN₅O₃
Molecular Weight: 539.68
Catalog: Signaling Pathways Apoptosis IAP
Create Date: 2018-04-13 06:04:02
Modify Date: 2026-07-01 18:50:57
ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).

Name	ASTX660
Synonyms	Tolinapant ASTX660(Tolinapant） 1-[6-[(4-Fluorophenyl)methyl]-2,3-dihydro-5-(hydroxymethyl)-3,3-dimethyl-1H-pyrrolo[3,2-b]pyridin-1-yl]-2-[(2R,5R)-5-methyl-2-[[(3R)-3-methyl-4-morpholinyl]methyl]-1-piperazinyl]ethanone Ethanone, 1-[6-[(4-fluorophenyl)methyl]-2,3-dihydro-5-(hydroxymethyl)-3,3-dimethyl-1H-pyrrolo[3,2-b]pyridin-1-yl]-2-[(2R,5R)-5-methyl-2-[[(3R)-3-methyl-4-morpholinyl]methyl]-1-piperazinyl] Inhibitor,inhibit,ASTX-660,ASTX660,IAP,ASTX ASTX660 (ASTX ASTX660, 10 mM in DMSO Tolinapant (ASTX660) 1-(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)ethanone

Description	ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
Related Catalog	Signaling Pathways >> Apoptosis >> IAP Research Areas >> Cancer
Target	cIAP, XIAP[1]
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	[1]. Tomoko Smyth, et al. Abstract 1287: The dual IAP antagonist, ASTX660, increases the anti-tumor activity of paclitaxel in preclinical models of triple-negative breast cancer in vivo. Cancer Res 2016;76(14 Suppl).