
ASTX660
CAS No. 1799328-86-1
ASTX660( ASTX 660 | ASTX-660 )
Catalog No. M12719 CAS No. 1799328-86-1
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.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
5MG | 132 | Get Quote |
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10MG | 205 | Get Quote |
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25MG | 410 | Get Quote |
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50MG | 605 | Get Quote |
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100MG | 860 | Get Quote |
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200MG | Get Quote | Get Quote |
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500MG | Get Quote | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameASTX660
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NoteResearch use only, not for human use.
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Brief DescriptionASTX660 is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM.
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DescriptionASTX660 is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM; potently inhibits association between XIAP and caspase 9 in HEK293 cell line with EC50 of 2.8 nM, binds to and leads to the degradation of cIAP1/2 and stabilisation of NIK in cell; induces apoptosis in MDA-MB-231 cells with EC50 of 1.8 nM, which is TNF-α-dependent; inhibits tumor growth in mice bearing breast and melanoma tumor xenografts.Blood Cancer Phase 2 Clinical(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.(In Vivo):In HCC1806 xenografts in mice, ASTX660 (daily oral treatment) causes moderate tumor growth inhibition but not regression.
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In VitroTolinapant 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 Tolinapant in vitro and it is found that 43% are sensitive to Tolinapant.
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In VivoIn HCC1806 xenografts in mice, Tolinapant (daily oral treatment) causes moderate tumor growth inhibition but not regression.
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SynonymsASTX 660 | ASTX-660
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PathwayApoptosis
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TargetIAP
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RecptorIAP
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Research AreaCancer
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IndicationBlood cancer
Chemical Information
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CAS Number1799328-86-1
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Formula Weight539.696
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Molecular FormulaC30H42FN5O3
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Purity>98% (HPLC)
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SolubilityDMSO : ≥ 50 mg/mL 92.65 mM
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SMILESCC1CN(C(CN1)CN2CCOCC2C)CC(=O)N3CC(C4=C3C=C(C(=N4)CO)CC5=CC=C(C=C5)F)(C)C
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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
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Ward GA, et al. Mol Cancer Ther. 2018 Apr 25. pii: molcanther.0848.2017.
molnova catalog



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