PI-103 | Potent inhibitor of PI-3 kinase, mTOR, and DNA-PK

A potent inhibitor of PI-3 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

  1. Knight et al. (2006), A Pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling; Cell, 125 733
  2. Raynaud et al. (2007), Pharmacologic characterization of a potent inhibitor of a class I phosphatidylinositide 3-kinases; Cancer Res., 67 5840
  3. 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
  4. Zou et al. (2009), A novel dual PI3Kalpha/mTOR inhibitor PI-103 with high antitumor activity in non-small cell lung cancer cells; J. Mol. Med. 24 97
  5. Fan et al. (2010), Akt and autophagy cooperate to promote survival of drug-resistant glioma; Signal., 3 ra81
  6. Hollerhage et al. (2019), Multiple molecular pathways stimulating macroautophagy protect from alpha-synuclein-induced toxicity in human neurons; Neuropharmacology, 149 13
Weight 0.01 mg
Dimensions 0.01 × 0.01 × 0.01 cm
Size:

5 mg, 25 mg

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CAS:
371935-74-9
Catalog Number:
10-5406
Activity:
Potent inhibitor of PI-3 kinase, mTOR and DNA-PK
Chemical Name:

3-[4-(4-Morpholinyl)pyrido[3’,2’:4,5]furo[3,2-d]pyrimidin-2-yl]-phenol

Molecular Weight:
348.36
Molecular Formula:
C19H16N4O3
Solubility:
Soluble in DMSO (up to 40 mg/ml)
Physical Properties:
White solid
Purity:
98% by TLC

NMR (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

PI-103 | Potent inhibitor of PI-3 kinase, mTOR, and DNA-PK

$60.00$240.00

CAS:
371935-74-9
Catalog Number:
10-5406
Activity:
Potent inhibitor of PI-3 kinase, mTOR and DNA-PK
Chemical Name:

3-[4-(4-Morpholinyl)pyrido[3’,2’:4,5]furo[3,2-d]pyrimidin-2-yl]-phenol

Molecular Weight:
348.36
Molecular Formula:
C19H16N4O3
Solubility:
Soluble in DMSO (up to 40 mg/ml)
Physical Properties:
White solid
Purity:
98% by TLC

NMR (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT
  • 5 mg
  • 25 mg
Clear
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SKU: 10-5406 Category: