PI-103
- Product Name
- PI-103
- CAS No.
- 371935-74-9
- Chemical Name
- PI-103
- Synonyms
- PI-103;PI 103;PI-103 - [P13259];PI 103 HYDROCHLORIDE;PI-103, 10 mM in DMSO;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
- CBNumber
- CB82454333
- Molecular Formula
- C19H16N4O3
- Formula Weight
- 348.36
- MOL File
- 371935-74-9.mol
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.
- InChI
- 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
- InChIKey
- TUVCWJQQGGETHL-UHFFFAOYSA-N
- SMILES
- C1(O)=CC=CC(C2=NC(N3CCOCC3)=C3OC4=NC=CC=C4C3=N2)=C1
N-Bromosuccinimide Price
- 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
- $177
- Updated
- 2025/07/31
- 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
- $650
- Updated
- 2025/07/31
- Product number
- 10009209
- Product name
- PI-103
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $30
- Updated
- 2024/03/01
- Product number
- 10009209
- Product name
- PI-103
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $113
- Updated
- 2024/03/01
- Product number
- 10009209
- Product name
- PI-103
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $169
- Updated
- 2024/03/01
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
[1] ZACHARY A KNIGHT. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling.[J]. Cell, 2006, 125 4: 733-747. DOI:10.1016/j.cell.2006.03.035
[2] FLORENCE I RAYNAUD. Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases.[J]. Cancer research, 2007, 67 12: 5840-5850. DOI:10.1158/0008-5472.can-06-4615
[3] ZHENYA HONG. Arsenic disulfide synergizes with the phosphoinositide 3-kinase inhibitor PI-103 to eradicate acute myeloid leukemia stem cells by inducing differentiation.[J]. Carcinogenesis, 2011, 32 10: 1550-1558. DOI:10.1093/carcin/bgr176
[4] ZU-QUAN ZOU. A novel dual PI3Kalpha/mTOR inhibitor PI-103 with high antitumor activity in non-small cell lung cancer cells.[J]. International journal of molecular medicine, 2009, 24 1: 97-101. DOI:10.3892/ijmm\_00000212
[5] QI-WEN FAN. Akt and Autophagy Cooperate to Promote Survival of Drug-Resistant Glioma[J]. Science Signaling, 2010, 3 147. DOI:10.1126/scisignal.2001017
[6] MATTHIAS HÖLLERHAGE . Multiple molecular pathways stimulating macroautophagy protect from alpha-synuclein-induced toxicity in human neurons[J]. Neuropharmacology, 2019, 149: Pages 13-26. DOI:10.1016/j.neuropharm.2019.01.023
PI-103 Preparation Products And Raw materials
Raw materials
Preparation Products
PI-103 Suppliers
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- 0550-5196001 15000891977
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- 86-10-82849933
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- 821-50328103-801 18930552037
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- 86-21-50328109
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View Lastest Price from PI-103 manufacturers
- Product
- PI-103 371935-74-9
- Price
- US $2.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2018-12-24