ChemicalBook > CAS DataBase List > PI-103

PI-103

Product Name
PI-103
CAS No.
371935-74-9
Chemical Name
PI-103
Synonyms
PI-103;PI 103;PI 103 HYDROCHLORIDE;PI-103, Free Base, >99%;PI-103HydrochlorideSalt;PI-103 - CAS 371935-74-9 - Calbiochem;PI 3-Kinase Inhibitor (PI-103) B-0303;PI-103, 98%, a potent PI3K/Akt and mTOR inhibitor;3-(4-Morpholinopyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl)phenol;3-(4-Morpholinopyrido[3',2':4,5] furo[3,2-d]pyriMidin-2-yl)phenol;3-[4-(4-Morpholinylpyrido[3',2',4,5]furo[3,2-d]pyrimidin-2-yl]phenol
CBNumber
CB82454333
Molecular Formula
C19H16N4O3
Formula Weight
348.36
MOL File
371935-74-9.mol
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PI-103 Property

Density 
1.409±0.06 g/cm3(Predicted)
storage temp. 
Keep in dark place,Sealed in dry,Store in freezer, under -20°C
solubility 
Soluble in DMSO (up to 40 mg/ml)
form 
White solid
pka
9.06±0.10(Predicted)
color 
White
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
528100
Product name
PI-103 - CAS 371935-74-9 - Calbiochem<br />A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR.
Packaging
1mg
Price
$172
Updated
2024/03/01
Sigma-Aldrich
Product number
528100
Product name
PI-103 - CAS 371935-74-9 - Calbiochem<br />A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR.
Packaging
5mg
Price
$632
Updated
2024/03/01
Cayman Chemical
Product number
10009209
Product name
PI-103
Purity
≥98%
Packaging
1mg
Price
$30
Updated
2024/03/01
Cayman Chemical
Product number
10009209
Product name
PI-103
Purity
≥98%
Packaging
5mg
Price
$113
Updated
2024/03/01
Cayman Chemical
Product number
10009209
Product name
PI-103
Purity
≥98%
Packaging
10mg
Price
$169
Updated
2024/03/01
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PI-103 Chemical Properties,Usage,Production

Description

PI-103 (371935-74-9) is a potent inhibitor of PI-3 kinase, mTOR and DNA-PK, IC50 = 8, 88, 150, 48,? 20, 83 and 2 nM for p110α, p110?, p110γ, p110δ, mTORC1, mTORC2 and DNA-PK respectively.1,2 Synergizes with arsenic disulfide to eradicate AML stem cells by induction of differentiation.3 Inhibits the growth of gefitinib-resistant non-small cell lung cancer cell lines.4 Induces autophagy in drug-resistant glioma.5 Protects against a-synuclein-induced toxicity in human neurons by induction of macroautophagy.6

Uses

PI 103 is a dual inhbitor of Class IA phosphatidylinositol 3-kinase and mammalian target of rapaymycin complex 1 (mTORC1), both of which are involved in pathways often activated in myelogenous leukemia. PI 103 also functions to enhance tumour radiosensitivity.

Definition

ChEBI: An organic heterotricyclic compound that is pyrido[3',2':4,5]furo[3,2-d]pyrimidine substituted at positions 2 and 4 by 3-hydroxyphenyl and morpholin-4-yl groups respectively. A dual-kinase inhibitor with anti-cancer properties.

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.

Biological Activity

Inhibitor of DNA-PK, PI 3-kinase (p110 α ) and mTOR (IC 50 values are 2, 8, 20, 26, 48, 83, 88, 150, 850, 920, ~ 1000 and 2300 nM for DNA-PK, p110 α , mTORC1, PI3KC2 β , p110 δ , mTORC2, p110 β , p110 γ , ATR, ATM, PI3KC2 α and hsVPS34 respectively). Inhibits growth of human tumor xenografts in mice in vivo .

Biochem/physiol Actions

Cell permeable: yes

target

Cell, 2013, 153(4):840-54

References

Knight et al. (2006), A Pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling; Cell, 125 733 Raynaud et al. (2007), Pharmacologic characterization of a potent inhibitor of a class I phosphatidylinositide 3-kinases; Cancer Res., 67 5840 Hong et al. (2011), Arsenic disulfide synergizes with the phosphoinositide 3-kinase inhibitor PI-103 to eradicate acute myeloid leukemia stem cells by inducing differentiation; Carcinogenesis, 32 1550 Zou et al. (2009), A novel dual PI3Kalpha/mTOR inhibitor PI-103 with high antitumor activity in non-small cell lung cancer cells; Int. J. Mol. Med. 24 97 Fan et al. (2010), Akt and autophagy cooperate to promote survival of drug-resistant glioma; Sci. Signal., 3 ra81 Hollerhage et al. (2019), Multiple molecular pathways stimulating macroautophagy protect from alpha-synuclein-induced toxicity in human neurons; Neuropharmacology, 149 13

PI-103 Preparation Products And Raw materials

Raw materials

Preparation Products

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PI-103 Suppliers

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View Lastest Price from PI-103 manufacturers

Career Henan Chemical Co
Product
PI-103 371935-74-9
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-24

371935-74-9, PI-103Related Search:


  • Phenol, 3-[4-(4-Morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyriMidin-2-yl]-
  • 3-(4-Morpholinopyrido[3',2':4,5] furo[3,2-d]pyriMidin-2-yl)phenol
  • PI 3-Kinase Inhibitor (PI-103) B-0303
  • PI-103, Free Base, >99%
  • PI-103 - CAS 371935-74-9 - Calbiochem
  • PI-103HydrochlorideSalt
  • 3-[4-(4-Morpholinylpyrido[3',2',4,5]furo[3,2-d]pyrimidin-2-yl]phenol
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  • PI 103 3-[4-(4-Morpholinylpyrido[3',2',4,5]furo[3,2-d]pyrimidin-2-yl]phenol
  • PI-103;PI 103
  • PI 103 HYDROCHLORIDE
  • 3-[4-Morpholin-4-ylpyrido[3',2':4,5]furo[3,2-d]pyriMidin-2-yl]phenol
  • PI-103, 98%, a potent PI3K/Akt and mTOR inhibitor
  • 3-[4-(4-MORPHOLINYLPYRIDO)[3',2':4,5]FURO[3,2-D]PYRIMIDIN-2-YL]PHENOL HYDROCHLORIDE
  • 3-[6-(morpholin-4-yl)-8-oxa-3,5,10-triazatricyclo[7.4.0.0^{2,7}]trideca-1(9),2(7),3,5,10,12-hexaen-4-yl]phenol
  • PI3K,Phosphoinositide 3-kinase,Inhibitor,DNA-PK,Apoptosis,Autophagy,DNA-dependent protein kinase,inhibit,PI-103,Mammalian target of Rapamycin,mTOR
  • 3-(4-Morpholinopyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl)phenol
  • 371935-74-9
  • C19H16N4O3HCl
  • Akt
  • mTOR
  • PI3K
  • Inhibitors