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ASTX660(Tolinapant）

  Cat. No.:  DC20695   Featured
Chemical Structure
1799328-86-1
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More than 5000 active chemicals with high quality for research!
Field of application
ASTX660 is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1799328-86-1
Chemical Name: 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)ethan-1-one
Synonyms: ASTX 660;ASTX-660
SMILES: C[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
Formula: C30H42FN5O3
M.Wt: 539.684590816498
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [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).
Description: ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
In Vivo: In HCC1806 xenografts in mice, ASTX660 (daily oral treatment) causes moderate tumor growth inhibition but not regression[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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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