PI-103
- CAS No.
- 371935-74-9
- Chemical Name:
- PI-103
- Synonyms
- PI-103;PI 103;PI 103 HYDROCHLORIDE;PI-103HydrochlorideSalt;PI-103, Free Base, >99%;PI 3-Kinase Inhibitor (PI-103) B-0303;PI-103 - CAS 371935-74-9 - Calbiochem;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
- Molecular Weight:
- 348.36
- MDL Number:
- MFCD11983145
- MOL File:
- 371935-74-9.mol
- MSDS File:
- SDS
| 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. |
| FDA UNII | YQX02F616F |
PI-103 price More Price(45)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | 528100 | PI-103 - CAS 371935-74-9 - Calbiochem A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR. |
371935-74-9 | 1mg | $172 | 2024-03-01 | Buy |
| Sigma-Aldrich | 528100 | PI-103 - CAS 371935-74-9 - Calbiochem A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR. |
371935-74-9 | 5mg | $632 | 2024-03-01 | Buy |
| Cayman Chemical | 10009209 | PI-103 ≥98% | 371935-74-9 | 1mg | $30 | 2024-03-01 | Buy |
| Cayman Chemical | 10009209 | PI-103 ≥98% | 371935-74-9 | 5mg | $113 | 2024-03-01 | Buy |
| Cayman Chemical | 10009209 | PI-103 ≥98% | 371935-74-9 | 10mg | $169 | 2024-03-01 | Buy |
PI-103 Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | sales@capotchem.com | China | 29797 | 60 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| career henan chemical co | +86-0371-86658258 | sales@coreychem.com | China | 29914 | 58 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22968 | 58 |
| Chongqing Chemdad Co., Ltd | +86-023-61398051 +8613650506873 | sales@chemdad.com | China | 39916 | 58 |
| Alchem Pharmtech,Inc. | 8485655694 | sales@alchempharmtech.com | United States | 63711 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49390 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
