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Submit ReviewPI 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.
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. 了解 Tocris 化合物库的更多信息。
分子量 | 384.82 |
公式 | C19H16N4O3.HCl |
储存 | Desiccate at +4°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 7.7 | 20 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: PI 103 hydrochloride, PI 103 hydrochloride supplier, inhibitors, inhibits, DNA-PK, mTOR, PI, 3-kinase, DNA-Dependent, Protein, Kinases, Mammalian, Target, Rapamycin, PI103, hydrochloride, 3-Kinase, DNA-dependent, Kinase, Inositol, Lipids, Checkpoint, Control, Autophagy, 2930, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PI 103 hydrochloride 的部分引用包括:
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
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