PI-103 | Potent inhibitor of PI3-kinase, mTOR, and DNA-PK
3-[4-(4-Morpholinyl)pyrido[3’,2’:4,5]furo[3,2-d]pyrimidin-2-yl]-phenol
98% by TLC
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $60.00 | ||
| 25 mg | $240.00 |
PI-103 (371935-74-9) is a potent inhibitor of PI3-kinase, mTOR and DNA-PK, IC50 = 8, 88, 150, 48, 20, 83 and 2 nM for p110α, p110ß, 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
References/Citations:
- 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
3-[4-(4-Morpholinyl)pyrido[3’,2’:4,5]furo[3,2-d]pyrimidin-2-yl]-phenol
98% by TLC
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
PI-103 (371935-74-9) is a potent inhibitor of PI3-kinase, mTOR and DNA-PK, IC50 = 8, 88, 150, 48, 20, 83 and 2 nM for p110α, p110ß, 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
References/Citations:
- 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
Related products
-
MitoBloCK-12 | Mitochondrial import inhibitor
From $40.00CAS:522-51-0Catalog Number:10-1525Activity:Mitochondrial import inhibitorChemical Name:1,1’-Decamethylenebis(4-aminoquinaldinium)dichlorideAlternate Name:Dequalinium chloride; MB12; DECAMolecular Weight:527.58Molecular Formula:C30H40Cl2N4Solubility:Soluble in DMSO (up to 1 mg/ml with warming) or in Water (up to 1 mg/ml)Physical Properties:Beige solidPurity:98% by TLC
NMR (Conforms)Storage Temperature:RTStability:Stable for 2 years as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 3 months.Shipping Code:RT -
TCEP HCl | Reducing agent
From $35.00CAS:51805-45-9Catalog Number:10-2961Activity:Reducing agentChemical Name:Tris(-Carboxyethyl)phosphine HClMolecular Weight:286.65Molecular Formula:C9H15O6P • HClSolubility:Soluble in Water (up to 50 mg/ml)Physical Properties:White solidPurity:99% by TLC
NMR (Conforms)Storage Temperature:-20°CStability:Stable for 1 year from date of purchase as supplied. Solutions in distilled water may be stored at -20°C for up to 1 month.Shipping Code:RT -
Rucaparib phosphate | PARP1 inhibitor
From $70.00CAS:459868-92-9Catalog Number:10-3321Activity:PARP1 inhibitorChemical Name:8-Fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-oneAlternate Name:AG-14699; PF01367338Molecular Weight:421.36Molecular Formula:C19H18FN3O • H3PO4Solubility:Soluble in DMSO (up to 25 mg/ml).Physical Properties:Yellow solidPurity:98% by HPLC
NMR (Conforms)Storage Temperature:-20°Stability:Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.Shipping Code:RT
Calculate the molar concentration, mass or volume in a solution.
Concentration × Volume × Molecular Weight = Mass
