Serabelisib (INK-1117,MLN-1117,TAK-117)

Catalog No.S8581

Serabelisib (INK-1117,MLN-1117,TAK-117) Chemical Structure

Molecular Weight(MW): 363.37

Serabelisib (INK-1117,MLN-1117,TAK-117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase.

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Biological Activity

Description Serabelisib (INK-1117,MLN-1117,TAK-117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase.
Targets
PI3Kα [1]
(Cell-free assay)
21 nM
In vitro

TAK-117 administration in PIK3CA-mutant tumor cell lines results in potent PI3K pathway inhibition, blockade of cellular proliferation, and apoptosis[1]. INK1117 potently inhibits PI3K and demonstrates a greater than 100-fold selectivity relative to other class I PI3K family members and mTOR as well as a high degree of selectivity against a large panel of protein kinases. INK1117 blocks proliferation of tumor cell lines bearing PIK3CA mutations, and inhibits cellular phosphorylation and activity of AKT. However, INK1117 shows much less activity in PTEN-deficient tumor cells, which typically display constitutive PI3K pathway activation independent of PI3Kα[3].

In vivo Administration of TAK-117 leads to dose-dependent inhibition of tumor growth in murine xenograft models of human cancer (e.g., breast carcinoma) bearing PIK3CA oncogenic mutations, with corresponding inhibition of PI3K pharmacodynamic markers in tumor tissue. Preclinical antitumor activity of single-agent TAK-117 has been shown to be independent of dosing schedules and driven by total plasma exposures. Conversely, TAK-117 is not efficacious in tumor models harboring PTEN and/or KRAS mutations. Preclinical studies show TAK-117 to have low potential for disrupting glucose metabolism or for causing cardiac adverse events; in rats and monkeys, doses up to 50 mg/kg/day were well tolerated. In human, The mean terminal half-life of TAK-117 is approximately 11 hours (range, 6-14 hours). There is no meaningful accumula-tion of TAK-117 with repeated dosing for any schedule[1]. Additionally, INK1117 does not significantly impair B and T cell function in vitro and in vivo[3].

Protocol

Cell Research:

[2]

+ Expand
  • Cell lines: NK cells
  • Concentrations: 20 min
  • Incubation Time: 1 μM
  • Method:

    --


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: C57BL/6 mice
  • Formulation: --
  • Dosages: 60 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 16 mg/mL (44.03 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck 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.

Chemical Information

Molecular Weight 363.37
Formula

C19H17N5O3

CAS No. 1268454-23-4
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID