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T-3256336

CAS No. 1266227-69-3

T-3256336( T3256336 | T 3256336 )

Catalog No. M11118 CAS No. 1266227-69-3

A potent, selective, orally available IAP antagonist with IC50 of 1.3, 2.2 and 200 nM for cIAP-1, cIAP-2 and XIAP, respectively.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    T-3256336
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective, orally available IAP antagonist with IC50 of 1.3, 2.2 and 200 nM for cIAP-1, cIAP-2 and XIAP, respectively.
  • Description
    A potent, selective, orally available IAP antagonist with IC50 of 1.3, 2.2 and 200 nM for cIAP-1, cIAP-2 and XIAP, respectively; dose dependently antagonizes XIAP and promotes the activities of caspase-3 with EC50 of 1.3 uM in cell-free assays, induces the rapid proteasomal degradation of cIAP-1 and activates TNF-α-dependent extrinsic apoptosis signaling in cultured cells; induces cIAP-1 degradation, TNF-α production and caspase activation in cancer xenograft models.
  • In Vitro
    ——
  • In Vivo
    Animal Model:Female BALB/cAJcl mice (MDA-MB-231-Luc xenograft)Dosage:30, 100 mg/kg Administration:P.o.Result:Stimulated caspase-3/7 activity in a dose-dependent manner, induced tumor regression in a dose-dependent manner with a percent tumor growth inhibition (T/C) of 53% and 62% at 30 mg/kg and 100 mg/kg, respectively.
  • Synonyms
    T3256336 | T 3256336
  • Pathway
    Apoptosis
  • Target
    IAP
  • Recptor
    IAP
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1266227-69-3
  • Formula Weight
    605.728
  • Molecular Formula
    C31H45F2N5O5
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O=C([C@H]1N(C([C@H](C2CCC(F)(F)CC2)NC([C@H](C)NC)=O)=O)C[C@](C[C@@H](OCC)C3)([H])N3C1)N[C@@H]4CCOC5=C4C=CC=C5
  • Chemical Name
    Pyrrolo[1,2-a]pyrazine-3-carboxamide, 2-[(2S)-2-(4,4-difluorocyclohexyl)-2-[[(2S)-2-(methylamino)-1-oxopropyl]amino]acetyl]-N-[(4R)-3,4-dihydro-2H-1-benzopyran-4-yl]-7-ethoxyoctahydro-, (3S,7R,8aR)-

Shipping & Storage Information

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

Reference

1. Sumi H, et al. Mol Cancer Ther. 2013 Feb;12(2):230-40. 2. Hashimoto K, et al. J Med Chem. 2013 Feb 14;56(3):1228-46. 3. Sumi H, et al. Biochem Biophys Res Commun. 2016 Oct 14;479(2):179-185.
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