Serabelisib (TAK-117)

Catalog No.S8581 Synonyms: INK-1117, MLN-1117

For research use only.

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

Serabelisib (TAK-117) Chemical Structure

CAS No. 1268454-23-4

Selleck's Serabelisib (TAK-117) has been cited by 3 Publications

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Biological Activity

Description Serabelisib (TAK-117, INK-1117, MLN-1117) 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 (from reference)

Cell Research:

[2]

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

    --

Animal Research:

[2]

  • Animal Models: C57BL/6 mice
  • Dosages: 60 mg/kg
  • Administration: oral

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 363.37
Formula

C19H17N5O3

CAS No. 1268454-23-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1COCCN1C(=O)C2=CN=C3N2C=C(C=C3)C4=CC5=C(C=C4)OC(=N5)N

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05300048 Recruiting Drug: Serabelisib|Other: Insulin Suppressing Diet Advanced Solid Tumor|PIK3CA Mutation|PTEN Loss of Function Mutation Faeth Therapeutics April 22 2022 Phase 1
NCT02625259 Completed Drug: TAK-117|Drug: Lansoprazole Neoplasm Advanced or Metastatic Millennium Pharmaceuticals Inc.|Takeda January 8 2016 Phase 1
NCT02393209 Terminated Drug: Docetaxel|Drug: TAK-117 Non-small Cell Lung Cancer Millennium Pharmaceuticals Inc.|Takeda June 3 2015 Phase 1|Phase 2
NCT01899053 Completed Drug: TAK-228|Drug: TAK-117 Advanced Nonhematologic Malignancies Millennium Pharmaceuticals Inc.|Takeda June 28 2013 Phase 1
NCT01449370 Completed Drug: TAK-117 Metastatic Solid Tumors Millennium Pharmaceuticals Inc.|Takeda October 2011 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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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