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Serabelisib

Cat. No. M6175
Serabelisib Structure
Synonym:

INK-1117,MLN-1117,TAK-117

Size Price Availability Quantity
10mg USD 150 In stock
25mg USD 320 In stock
50mg USD 520 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: TAK-117 administration in PIK3CA-mutant tumor cell lines results in potent PI3K pathway inhibition, blockade of cellular proliferation, and apoptosis. 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.

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. Additionally, INK1117 does not significantly impair B and T cell function in vitro and in vivo.

Protocol
Cell Experiment
Cell lines NK cells
Preparation method
Concentrations 1 μM
Incubation time 20 min
Animal Experiment
Animal models C57BL/6 mice
Formulation
Dosages 60 mg/kg
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 363.37
Formula C19H17N5O3
CAS Number 1268454-23-4
Purity >99%
Solubility 16 mg/mL in DMSO
Storage at -20°C
References

A First-in-Human, Phase I, Dose-Escalation Study of TAK-117, a Selective PI3Kα Isoform Inhibitor, in Patients with Advanced Solid Malignancies.
Juric D, et al. Clin Cancer Res. 2017 Sep 1;23(17):5015-5023. PMID: 28490463.

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Keywords: Serabelisib, INK-1117,MLN-1117,TAK-117 supplier, PI3K, inhibitors

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