- PI-103
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- $52.00 / 5mg
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2025-07-15
- CAS:371935-74-9
- Min. Order:
- Purity: 99.3%
- Supply Ability: 10g
- PI-103
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- $2.00 / 1kg
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2019-07-06
- CAS:371935-74-9
- Min. Order: 1kg
- Purity: 99%
- Supply Ability: 100kg
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| Product Name: | PI-103 | | Synonyms: | 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 | | CAS: | 371935-74-9 | | MF: | C19H16N4O3 | | MW: | 348.36 | | EINECS: | | | Product Categories: | Akt;mTOR;PI3K;Inhibitors | | Mol File: | 371935-74-9.mol |  |
| | PI-103 Chemical Properties |
| 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 |
| | PI-103 Usage And Synthesis |
| 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 |
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