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

China 129 Germany 1 India 1 The Netherlands 1 United Kingdom 2 United States 25 Global 159

Chuzhou KeMail Chemical Technology Co., Ltd

Tel: 0550-5196001 15000891977
Fax: 0550-5196001
Email: wj520wjxby@126.com
Country: China
ProdList: 1832
Advantage: 55

Shanghai Boyle Chemical Co., Ltd.

Tel
Fax: 86-21-57758967
Email: sales@boylechem.com
Country: China
ProdList: 2923
Advantage: 55

J & K SCIENTIFIC LTD.

Tel: 010-82848833 400-666-7788
Fax: 86-10-82849933
Email: jkinfo@jkchemical.com
Country: China
ProdList: 96815
Advantage: 76

3B Pharmachem (Wuhan) International Co.,Ltd.

Tel: 821-50328103-801 18930552037
Fax: 86-21-50328109
Email: 3bsc@sina.com
Country: China
ProdList: 15848
Advantage: 69

Chembest Research Laboratories Limited

Tel: 021-20908456
Fax: 021-58180499
Email: sales@BioChemBest.com
Country: China
ProdList: 6011
Advantage: 61

Shanghai Yuanding Chem. Sci. & Tech. Co., Ltd.

Tel: 21-57721279
Fax: QQ：14057904
Email: sales@shydchem.com.cn
Country: China
ProdList: 982
Advantage: 56

Shangchem Co., Ltd.

Tel: +86-21-68182121
Fax: +86-21-68182121
Country: China
ProdList: 882
Advantage: 52

Nanjing Chemlin Chemical Co., Ltd

Tel: 025-83697070
Fax: +86-25-83453306
Email: info@chemlin.com.cn
Country: China
ProdList: 17987
Advantage: 64

Chemsky (shanghai) International Co.,Ltd

Tel: 021-50135380
Email: shchemsky@sina.com
Country: China
ProdList: 15421
Advantage: 60

Jinan Trio PharmaTech Co., Ltd.

Tel: +86 (531) 88811783
Fax: +86 (531) 55696010 QQ 1762738062
Email: sales@trio-pharmatech.com (International market)
Country: China
ProdList: 1856
Advantage: 62

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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:

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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

3-(4-morpholinopyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl)phenol hydrochloride

3-[4-(4-Morpholinylpyrido[3',2',4,5]furo[3,2-d]pyrimidin-2-yl]phenol PI 103

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