TSU-68 (Orantinib, SU6668)Catalog No. A10953

Quick Overview

Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.
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TSU-68 (Orantinib, SU6668)

TSU-68 (Orantinib, SU6668)  Citations(1)
  • Aaron Y. Lai,et al. Venular degeneration leads to vascular dysfunction in a transgenic model of Alzheimer's disease., Brain, 2015, Apr;138(Pt 4):1046-58 25688079
  • Product Information
    Catalog Num A10953
    M. Wt 310.4
    Formula C18H18N2O3
    Solubility DMSO
    Purity >98%
    Storage at -20°C 3 years Powder
    CAS No. 252916-29-3
    Synonyms TSU68
    Chemical Name 5-[1,2-Dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-propanoic acid
    SMILES Code CC1=C(NC(=C1CCC(=O)O)C)/C=C\2/C3=CC=CC=C3NC2=O

    Biological activity
    Introduction
    Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.
    Targets
    PDGFRβ (Cell-free assay) FGFR1 (Cell-free assay) Flk1 (Cell-free assay)
    8 nM(Ki)1.2 μM(Ki)2.1 μM(Ki)
    Solubility
    Solubility (25C) * In vitro DMSO 62 mg/mL (199.77 mM)
    Water <1 mg/mL (<1 mM)
    Ethanol <1 mg/mL (<1 mM)
    In vivo 1% DMSO/30% polyethylene glycol/1% Tween 80 30 mg/mL
    * <1 mg/ml means slightly soluble or insoluble.
    * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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