P-9099 PI-103, Free Base, >99%

Synonyms : [PI3-Kinase α Inhibitor I]

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  • 10 mg
  • 52
  • 47
  • 42
  • 6,700
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  • In stock
  • 25 mg
  • 117
  • 107
  • 94
  • 15,200
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  • 50 mg
  • 199
  • 183
  • 160
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  • 100 mg
  • 358
  • 329
  • 289
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  • 200 mg
  • 614
  • 564
  • 496
  • 79,700
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  • M.W. 348.36
  • C19H16N4O3
  • [371935-74-9]

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO. Disposal: A.

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  • PI-103 is a dual inhibitor of class IA phosphatidylinositide 3-kinase (PI3K) and mTOR. PI3K is a class of lipid kinases that phosphorylate phosphatidylinositol 4,5-bisphosphate (PIP2) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 activates Akt and mTOR, and plays important roles in cell growth and survival.
  • This research compound is the free base form of PI-103. We also plan to offer the HCl salt form; please see PI-103, Hydrochloride Salt, Cat. No. P-9088. The hydrochloride salt form will be added to our website as soon as the first lot is ready.
  • PI-103 is a potent and selective PI3K inhibitor with low IC50 values against PI3K isoforms p110α (2 nM), p110β (3 nM), p110δ (3 nM), and p110γ (15 nM). PI-103 at 0.5 µM also inhibited TORC1 by 84% and demonstrated an IC50 of 14 nM against DNA-PK. PI-103 potently inhibited proliferation and invasion of a wide variety of human cancer cells in vitro and induced tumor growth delay in eight different human cancer xenograft models. PI-103 also demonstrated antiangiogenic potential. Raynaud F.I., et al. "Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases." Cancer Res. 67: 5840-5850 (2007).
  • PI-103 had antitumor activity in two gefitinib-resistant (please see Cat. No. G-4408, Gefitinib, Free Base) non-small cell lung cancer cell lines, A549 and H460, possibly by simultaneously inhibiting p70s6k phosporylation and Akt phosphorylation due to mTOR inhibition. Zou Z.Q., et al. "A novel dual PI3Kalpha/mTOR inhibitor PI-103 with high antitumor activity in non-small cell lung cancer cells." Int. J. Mol. Med. 24: 97-101 (2009).
  • PI-103 was mainly cytostatic for human leukemic cell lines and induced cell cycle arrest in the G1 phase. In blast cells from AML patients, PI-103 inhibited leukemic proliferation and the clonogenicity of leukemic progenitors, and induced mitochondrial apoptosis. Park S., et al. "PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase and mTOR, has antileukemic activity in AML." Leukemia 22: 1698-1706 (2008).
  • PI-103 inhibited the proliferation of glioma cells, possibly by its ability to inhibit both PI3 kinaseα and mTOR. It showed significant inhibitory activity in xenografted tumors with no observable toxicity. Fan Q.W., et al. "A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma." Cancer Cell 9: 341-349 (2006).
  • A combined treatment with arsenic disulfide and PI-103 synergistically killed non-acute promyelocytic leukemia cells and promoted their differentiation in vitro. Hong Z., et al. "Arsenic disulfide synergizes with the phosphoinositide 3-kinase inhibitor PI-103 to eradicate acute myeloid leukemia stem cells by inducing differentiation." Carcinogenesis 32: 1550-1558 (2011).
  • PI-103 inhibited endothelial cell proliferation and survival in vitro and tumor growth in vivo possibly by blocking activation of both PI3K and mTOR in vGPCR-expressing endothelial cells. Chaisuparat R., et al. "Dual inhibition of PI3Kα and mTOR as an alternative treatment for Kaposi's sarcoma." Cancer Res. 68: 8361-8368 (2008).
  • This PI-103 product is the free base form, whose CAS number is given above. The CAS number of the hydrochloride salt form is 371935-79-4.
  • Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.