GDC-0152

CAS No. 873652-48-3

GDC-0152( —— )

Catalog No. M16352 CAS No. 873652-48-3

GDC-0152 is a potent antagonist of XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 28 nM, 14 nM, 17 nM and 43 nM, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GDC-0152
  • Note
    Research use only, not for human use.
  • Brief Description
    GDC-0152 is a potent antagonist of XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 28 nM, 14 nM, 17 nM and 43 nM, respectively.
  • Description
    GDC-0152 is a potent antagonist of XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 28 nM, 14 nM, 17 nM and 43 nM, respectively; less affinity shown to cIAP1-BIR2 and cIAP2-BIR2. Phase 1. (In Vivo):GDC-0152 has moderate predicted hepatic clearance based on metabolic stability assays conducted using human liver microsomes. Plasma?protein binding of GDC-0152 is moderate and comparable among mice (88?91%), rats (89?91%), dogs (81?90%), monkeys (76?85%), and humans (75?83%) over the range of concentrations investigated (0.1?100 μM); higher plasma?protein binding is observed in rabbits (95?96%). GDC-0152 does not preferentially distribute to red blood cells with blood?plasma partition ratios ranging from 0.6 to 1.1 in all species tested. The pharmacokinetics for GDC-0152 is achieved with a C max of 53.7 μM and AUC of 203.5 h·μM.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Apoptosis
  • Target
    IAP
  • Recptor
    cIAP1-BIR3| cIAP2-BIR3| MLXBIR3SG| XIAP-BIR2| XIAP-BIR3
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    873652-48-3
  • Formula Weight
    498.64
  • Molecular Formula
    C25H34N6O3S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:99 mg/mL (198.54 mM); Ethanol:99 mg/mL (198.54 mM); Water:3 mg/mL (6.01 mM)
  • SMILES
    CN[C@@H](C)C(=O)N[C@@H](C1CCCCC1)C(=O)N1CCC[C@H]1C(=O)NC1=C(N=NS1)C1=CC=CC=C1 |r,c:28,34,36,t:26,32|
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.Flygare JA, et al. J Med Chem, 2012, 55(9), 4101-4113.
molnova catalog
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