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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    ASTX660
  • Note
    Research use only, not for human use.
  • Brief Description
    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.
  • Description
    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; 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.
  • In Vitro
    Tolinapant 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.
  • In Vivo
    In HCC1806 xenografts in mice, Tolinapant (daily oral treatment) causes moderate tumor growth inhibition but not regression.
  • Synonyms
    ASTX 660 | ASTX-660
  • Pathway
    Apoptosis
  • Target
    IAP
  • Recptor
    IAP
  • Research Area
    Cancer
  • Indication
    Blood cancer

Chemical Information

  • CAS Number
    1799328-86-1
  • Formula Weight
    539.696
  • Molecular Formula
    C30H42FN5O3
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : ≥ 50 mg/mL 92.65 mM
  • SMILES
    CC1CN(C(CN1)CN2CCOCC2C)CC(=O)N3CC(C4=C3C=C(C(=N4)CO)CC5=CC=C(C=C5)F)(C)C
  • 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

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Ward GA, et al. Mol Cancer Ther. 2018 Apr 25. pii: molcanther.0848.2017.
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