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Submit ReviewPI 103 hydrochloride
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)
Biological Activity for PI 103 hydrochloride
PI 103 hydrochloride is an 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 for PI 103 hydrochloride
PI 103 hydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for PI 103 hydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PI 103 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.7 | 20 |
Preparing Stock Solutions for PI 103 hydrochloride
The following data is based on the product molecular weight 384.82. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 12.99 mL | 64.97 mL | 129.93 mL |
| 1 mM | 2.6 mL | 12.99 mL | 25.99 mL |
| 2 mM | 1.3 mL | 6.5 mL | 12.99 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.6 mL |
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Product Datasheets for PI 103 hydrochloride
References for PI 103 hydrochloride
References are publications that support the biological activity of the product.
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 Ins 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
If you know of a relevant reference for PI 103 hydrochloride, please let us know.
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10 Citations for PI 103 hydrochloride
Citations are publications that use Tocris products. Selected citations for PI 103 hydrochloride include:
Guo et al (2017) Epigenetic resetting of human pluripotency. Development 144 2748 PMID: 28765214
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) OE and mTORC2 cooperate to enhance prostaglandin biosynthesis and tumorigenesis in TSC2-deficient LAM cells. Pain 211 15 PMID: 24395886
Makhortova et al (2011) A screen for regulators of survival of motor neuron protein levels. Nat Chem Biol 7 544 PMID: 21685895
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
Campbell et al (2013) P-Rex1 cooperates with PDGFRβ to drive cellular migration in 3D microenvironments. PLoS One 8 e53982 PMID: 23382862
Rostovskaya et al (2019) Capacitation of human naïve pluripotent stem cells for multi-lineage differentiation. Development 146 PMID: 30944104
Genga et al (2019) Single-Cell RNA-Sequencing-Based CRISPRi Screening Resolves Molecular Drivers of Early Human Endoderm Development. Cell Rep 27 708 PMID: 30995470
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? Please let us know.
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