PI 103 hydrochloride

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Cat.No. 2930 - PI 103 hydrochloride | C19H16N4O3.HCl | CAS No. 371935-79-4
Description: Inhibitor of PI 3-kinase, mTOR and DNA-PK
Chemical Name: 3-[4-(4-Morpholinylpyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (6)
Reviews
Literature

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.

Compound Libraries

PI 103 hydrochloride is also offered as part of the Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 384.82
Formula C19H16N4O3.HCl
Storage Desiccate at +4°C
Purity ≥98% (HPLC)
CAS Number 371935-79-4
PubChem ID 16739368
InChI Key XSQMYBFFYPTMFE-UHFFFAOYSA-N
Smiles OC1=CC(C(N=C4N5CCOCC5)=NC3=C4OC2=NC=CC=C23)=CC=C1.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 7.7 20

Preparing Stock Solutions

The following data is based on the product molecular weight 384.82. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.6 mL 12.99 mL 25.99 mL
5 mM 0.52 mL 2.6 mL 5.2 mL
10 mM 0.26 mL 1.3 mL 2.6 mL
50 mM 0.05 mL 0.26 mL 0.52 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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


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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, PI, 3-Kinase, mTOR, DNA-dependent, Protein, Kinase, Inositol, Lipids, Checkpoint, Control, Kinases, Autophagy, PI, 3-Kinase, Tocris Bioscience

6 Citations for PI 103 hydrochloride

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

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

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


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Literature in this Area

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