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526561 Sigma-Aldrich

PI 3-K/mTOR Inhibitor III, PKI-179 - CAS 1197160-28-3 - Calbiochem

The PI 3-K/mTOR Inhibitor III, PKI-179, also referenced under CAS 1197160-28-3, controls the biological activity of PI 3-K/mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym: PI 3-K/mTOR Inhibitor III, PKI-179 - CAS 1197160-28-3 - Calbiochem

  • CAS Number 1197160-28-3

  • Empirical Formula (Hill Notation) C25H28N8O3 · xH2O

  • Molecular Weight 488.54 (anhydrous basis)

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Properties

Related Categories Cell Biology, Cell Signaling and Neuroscience, Kinase/Phosphatase Biology, Mammalian target of Rapamycin (mTOR), Serine/Threonine Kinase Biology,
Quality Level   100
assay   ≥98% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  desiccated
  protect from light
storage conditions   +2C to +8C
color   white
solubility   DMSO: 50 mg/mL
shipped in   ambient

Description

General description

A cell-permeable triazinyl-phenyl-pyridiny

A cell-permeable triazinyl-phenyl-pyridinylurea compound that acts as a potent inhibitor against mTOR (IC = 0.42 nM) and PI 3-K (IC = 8, 24, 74, 77, 14, and 11 nM against isoform α, β, γ, δ, α E545K mutant, and α H1047R mutant, respectively) activities, exhibiting much reduced or little activity against a panel of 361 other kinases (IC >50 µM), Cytochrome CYP isoforms, or hERG. It is reported to be orally available in mouse, rat, monkey, and dog species, and effectively suppress cancer growth both in cultures in vitro (IC = 22 and 29 nM, respectively, against MDA361 and PC3mm2) and in mice in vivo (by 30% of control MDA361 tumor size on day 42; 50 mg/kg/day p.o.) via apoptosis induction as a result of Akt/mTOR pathway inhibition.

The PI 3-K/mTOR Inhibitor III, PKI-179, also referenced under CAS 1197160-28-3, controls the biological activity of PI 3-K/mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Venkatesan, A.M., et al. 2010. Bioorg. Med. Chem. Lett.20, 5869.
Chen, Z., et al. 2010. J. Org. Chem.75, 1643.

Safety & Documentation

Safety Information

Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable
Protocols & Articles
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