PI 103 hydrochloride

Cat. No. 2930

PI 103 hydrochloride C19H16N4O3.HCl [371935-79-4]

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Chemical Name: 3-[4-(4-Morpholinylpyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol hydrochloride

Biological Activity

Inhibitor of DNA-PK, PI 3-kinase (p110α) and mTOR (IC50 values are 2, 8, 20, 26, 48, 83, 88, 150, 850, 920, ~ 1000 and 2300 nM for DNA-PK, p110α, mTORC1, PI 3-KC2β, p110δ, mTORC2, p110β, p110γ, ATR, ATM, PI 3-KC2α and hsVPS34 respectively). Inhibits growth of human tumor xenografts in mice in vivo. Induces autophagosome formation in glioma cells.

Technical Data

M.Wt:
384.82
Formula:
C19H16N4O3.HCl
Solubility:
Soluble to 20 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at +4°C
CAS No:
371935-79-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Fan et al (2010) Akt and autophagy cooperate to promote survival of drug-resistant glioma. Sci.Signal. 3 ra81. PMID: 21062993.

Raynaud et al (2007) Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositol 3-kinase. Cancer Res. 67 5840. PMID: 17575152.

Fan et al (2006) A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer cell 9 341. PMID: 16697955.

Knight et al (2006) A pharmacological map of the PI3-K family defines a role for p110α in insulin signaling. Cell 125 733. PMID: 16647110.

If you know of a relevant reference for PI 103 hydrochloride please let us know.

Citations are publications that use Tocris products. Selected citations for PI 103 hydrochloride include:

Brown et al (2014) Mitogen-activated protein kinase-interacting kinase regulates mTOR/AKT signaling and controls the serine/arginine-rich protein kinase-responsive type 1 internal ribosome entry site-mediated translation and viral oncolysis. PLoS One 88 13149. PMID: 25187540.

Li et al (2014) Rapamycin-insensitive up-regulation of adipocyte phospholipase A2 in tuberous sclerosis and lymphangioleiomyomatosis. J Exp Med 9 e104809. PMID: 25347447.

Li et al (2014) Estradiol and mTORC2 cooperate to enhance prostaglandin biosynthesis and tumorigenesis in TSC2-deficient LAM cells. Pain 211 15. PMID: 24395886.

Campbell et al (2013) P-Rex1 cooperates with PDGFRβ to drive cellular migration in 3D microenvironments. PLoS One 8 e53982. PMID: 23382862.

Montané and Menand (2013) ATP-competitive mTOR kinase inhibitors delay plant growth by triggering early differentiation of meristematic cells but no developmental patterning change. J Virol 64 4361. PMID: 23963679.

Peng et al (2012) Platelet-derived growth factor CC-mediated neuroprotection against HIV Tat involves TRPC-mediated inactivation of GSK 3beta. PLoS One 7 e47572. PMID: 23077641.

Do you know of a great paper that uses PI 103 hydrochloride from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: PI 103 hydrochloride, supplier, inhibitors, inhibits, DNA-PK, mTOR, PI, 3-kinase, DNA-Dependent, Protein, Kinases, Mammalian, Target, Rapamycin, PI103, hydrochloride, Tocris Bioscience, PI 3-kinase Inhibitor products

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