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528100

PI-103

Name: PI-103
Brand: MM

≥97% (HPLC), PI3-K inhibitor, solid

Synonym(s):

PI-103, 3-(4-(4-Morpholinyl)pyrido[3ʹ,2ʹ:4,5]furo[3,2-d]pyrimidin-2-yl)phenol, mTOR Inhibitor V, PI 3-K Inhibitor V

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About This Item

Empirical Formula (Hill Notation):

C₁₉H₁₆N₄O₃

CAS Number:

371935-74-9

Molecular Weight:

348.36

MDL number:

MFCD11983145

UNSPSC Code:

12352200

NACRES:

NA.77

Assay:

≥97% (HPLC)

Form:

solid

Storage condition:

OK to freeze, protect from light

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Properties

Product Name

PI-103, A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR.

Quality Segment

100

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

−20°C

SMILES string

N5(CCOCC5)c1nc(nc3c1[o]c4ncccc43)c2cc(ccc2)O

InChI

1S/C19H16N4O3/c24-13-4-1-3-12(11-13)17-21-15-14-5-2-6-20-19(14)26-16(15)18(22-17)23-7-9-25-10-8-23/h1-6,11,24H,7-10H2

InChI key

TUVCWJQQGGETHL-UHFFFAOYSA-N

Description

General description

A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR (IC₅₀ = 2, 8, 88, 48, 150, 26, 20, and 83 nM for DNA-PK, p110α, p110β, p110δ, p110γ, PI3-KC2β, mTORC1, and mTORC2, respectively). It inhibits ATR and ATM only at much higher concentrations (IC₅₀ = 850 and 920 nM, respectively) and exhibits little activity towards a panel of more than 40 other kinases even at concentrations as high as 10 µM. Shown to effectively block PI3-K/Akt signaling and cell proliferation in glioma cell lines both in vitro and in vivo. A 10 mM (2 mg/574 µl) solution of PI-103 (Cat. No. 528101) in DMSO is also available.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
DNA-PK, PI3-K, and mTOR

Product competes with ATP.

Reversible: no

Target IC₅₀: 2, 8, 88, 48, 150, 26, 20, and 83 nM for DNA-PK, p110α, p110β, p110delta;, p110γ, PI3-KC2β, mTORC1, and mTORC2, respectively

Packaging

Packaged under inert gas

Preparation Note

Slight warming may be required for complete solubilization.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c