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MedKoo Cat#: 202235 | Name: PI-103
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110α), and mTOR.

Chemical Structure

PI-103
PI-103
CAS#371935-74-9 (free base)

Theoretical Analysis

MedKoo Cat#: 202235

Name: PI-103

CAS#: 371935-74-9 (free base)

Chemical Formula: C19H17ClN4O3

Exact Mass: 384.0989

Molecular Weight: 384.82

Elemental Analysis: C, 59.30; H, 4.45; Cl, 9.21; N, 14.56; O, 12.47

Price and Availability

Size Price Availability Quantity
10mg USD 285.00 2 Weeks
50mg USD 550.00 2 Weeks
100mg USD 950.00 2 Weeks
200mg USD 1,650.00 2 Weeks
500mg USD 3,250.00 2 Weeks
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Related CAS #
371935-74-9 (free base); 371935-79-4 (HCl)
Synonym
PI103; PI-103; PI 103.
IUPAC/Chemical Name
3-(4-morpholinopyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl)phenol
InChi Key
TUVCWJQQGGETHL-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H16N4O3/c24-13-4-1-3-12(11-13)17-21-15-14-5-2-6-20-19(14)26-16(15)18(22-17)23-7-9-25-10-8-23/h1-6,11,24H,7-10H2
SMILES Code
OC1=CC=CC(C2=NC(N3CCOCC3)=C(OC4=NC=CC=C45)C5=N2)=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Related CAS# 371935-74-9 (free base); 371935-79-4 (HCl)    
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM.
In vitro activity:
PI-103 is a new potent PI3K/Akt and mTOR inhibitor. In human leukemic cell lines and in primary blast cells from AML patients, PI-103 inhibited constitutive and growth factor-induced PI3K/Akt and mTORC1 activation. PI-103 was essentially cytostatic for cell lines and induced cell cycle arrest in the G1 phase. In blast cells, PI-103 inhibited leukemic proliferation, the clonogenicity of leukemic progenitors and induced mitochondrial apoptosis, especially in the compartment containing leukemic stem cells. Reference: Leukemia. 2008 Sep;22(9):1698-706. https://pubmed.ncbi.nlm.nih.gov/18548104/
In vivo activity:
This study evaluated the therapeutic efficacy of a novel PI3-kinase/mTOR inhibitor, PI-103, in established glioma lines and primary CD133(+) glioma-initiating cells and explored the potential of combining PI-103 with stem cell-delivered secretable tumor necrosis factor apoptosis-inducing ligand (S-TRAIL) both in vitro and in orthotopic mouse models of gliomas. This study shows that PI-103 inhibits proliferation and invasion, causes G(0)-G(1) arrest in cell cycle, and results in significant attenuation of orthotopic tumor growth in vivo in mice. Reference: Cancer Res. 2011 Jan 1;71(1):154-63. https://pubmed.ncbi.nlm.nih.gov/21084267/
Solvent mg/mL mM
Solubility
DMF 10.0 28.71
DMSO 16.3 42.44
DMSO:PBS (pH 7.2) (1:2) 0.3 0.65
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Park S, Chapuis N, Bardet V, Tamburini J, Gallay N, Willems L, Knight ZA, Shokat KM, Azar N, Viguié F, Ifrah N, Dreyfus F, Mayeux P, Lacombe C, Bouscary D. PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase and mTOR, has antileukemic activity in AML. Leukemia. 2008 Sep;22(9):1698-706. doi: 10.1038/leu.2008.144. Epub 2008 Jun 12. PMID: 18548104. 2. Fan QW, Knight ZA, Goldenberg DD, Yu W, Mostov KE, Stokoe D, Shokat KM, Weiss WA. A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell. 2006 May;9(5):341-9. doi: 10.1016/j.ccr.2006.03.029. PMID: 16697955; PMCID: PMC2925230. 3. Bagci-Onder T, Wakimoto H, Anderegg M, Cameron C, Shah K. A dual PI3K/mTOR inhibitor, PI-103, cooperates with stem cell-delivered TRAIL in experimental glioma models. Cancer Res. 2011 Jan 1;71(1):154-63. doi: 10.1158/0008-5472.CAN-10-1601. Epub 2010 Nov 17. PMID: 21084267.
In vitro protocol:
1. Park S, Chapuis N, Bardet V, Tamburini J, Gallay N, Willems L, Knight ZA, Shokat KM, Azar N, Viguié F, Ifrah N, Dreyfus F, Mayeux P, Lacombe C, Bouscary D. PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase and mTOR, has antileukemic activity in AML. Leukemia. 2008 Sep;22(9):1698-706. doi: 10.1038/leu.2008.144. Epub 2008 Jun 12. PMID: 18548104. 2. Fan QW, Knight ZA, Goldenberg DD, Yu W, Mostov KE, Stokoe D, Shokat KM, Weiss WA. A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell. 2006 May;9(5):341-9. doi: 10.1016/j.ccr.2006.03.029. PMID: 16697955; PMCID: PMC2925230.
In vivo protocol:
1. Bagci-Onder T, Wakimoto H, Anderegg M, Cameron C, Shah K. A dual PI3K/mTOR inhibitor, PI-103, cooperates with stem cell-delivered TRAIL in experimental glioma models. Cancer Res. 2011 Jan 1;71(1):154-63. doi: 10.1158/0008-5472.CAN-10-1601. Epub 2010 Nov 17. PMID: 21084267.
1: Saha T, Fojtů M, Nagar AV, Thurakkal L, Srinivasan BB, Mukherjee M, Sibiyon A, Aggarwal H, Samuel A, Dash C, Jang HL, Sengupta S. Antibody nanoparticle conjugate-based targeted immunotherapy for non-small cell lung cancer. Sci Adv. 2024 Jun 14;10(24):eadi2046. doi: 10.1126/sciadv.adi2046. Epub 2024 Jun 14. PMID: 38875335; PMCID: PMC11177938. 2: Wan B, Zhang W, Deng X, Lu Y, Zhang Z, Yang Y. Molecular Expression and Prognostic Implications of Krüppel-Like Factor 3 (KLF3) in Clear Cell Renal Cell Carcinoma. Crit Rev Eukaryot Gene Expr. 2024;34(2):45-59. doi: 10.1615/CritRevEukaryotGeneExpr.2023049010. PMID: 38073441. 3: Dong YQ, Sun N, Yang XC, He MQ, Huang H, Guo WJ, Lin XJ. Suppression of Autophagy Can Augment PIK3 Inhibitor Induced Apoptosis in T Lymphoblastic Leukemia Cell Lines. Ann Clin Lab Sci. 2023 Jul;53(4):598-606. PMID: 37625845. 4: Kumar R, Kumar A, Kumar A, Singh AK, Kumar P. Design, Synthesis and Molecular Docking Studies of Pyrazoline Derivatives as PI3K Inhibitors. Comb Chem High Throughput Screen. 2024;27(2):256-272. doi: 10.2174/1386207326666230504163312. PMID: 37143279. 5: Kano M, Nishibe T, Matsumoto R, Fujiyoshi T, Toya N, Dardik A, Ogino H. Significance of perioperative intrasac pressure in sac shrinkage after endovascular abdominal aneurysm repair. Int Angiol. 2023 Jun;42(3):201-208. doi: 10.23736/S0392-9590.23.05004-6. Epub 2023 Apr 17. PMID: 37067390. 6: Patel H, Mishra R, Wier A, Mokhtarpour N, Merino EJ, Garrett JT. RIDR-PI-103, ROS-activated prodrug PI3K inhibitor inhibits cell growth and impairs the PI3K/Akt pathway in BRAF and MEK inhibitor-resistant BRAF-mutant melanoma cells. Anticancer Drugs. 2023 Apr 1;34(4):519-531. doi: 10.1097/CAD.0000000000001500. Epub 2023 Feb 10. PMID: 36847042; PMCID: PMC9997637. 7: El-Daly SM, Abo-Elfadl MT, Hussein J, Abo-Zeid MAM. Enhancement of the antitumor effect of 5-fluorouracil with modulation in drug transporters expression using PI3K inhibitors in colorectal cancer cells. Life Sci. 2023 Feb 15;315:121320. doi: 10.1016/j.lfs.2022.121320. Epub 2022 Dec 24. PMID: 36574946. 8: Chen LF, Xu WB, Xiong S, Cai JX, Zhang JJ, Li YL, Li MM, Zhang H, Liu Z. PIK-24 Inhibits RSV-Induced Syncytium Formation via Direct Interaction with the p85α Subunit of PI3K. J Virol. 2022 Dec 14;96(23):e0145322. doi: 10.1128/jvi.01453-22. Epub 2022 Nov 23. PMID: 36416586; PMCID: PMC9749462. 9: Chen Y, Wu T, Yang C, Lu M, Chen Z, Deng M, Jia Y, Yang Y, Liu X, Wang H, Ling Y, Lu L, Zhou Y. A pyridinesulfonamide derivative FD268 suppresses cell proliferation and induces apoptosis via inhibiting PI3K pathway in acute myeloid leukemia. PLoS One. 2022 Nov 22;17(11):e0277893. doi: 10.1371/journal.pone.0277893. PMID: 36413544; PMCID: PMC9681083. 10: Zhu WZ, Feng DC, Xiong Q, Shi X, Zhang FC, Wei Q, Yang L. An autophagy- related gene prognostic index predicting biochemical recurrence, metastasis, and drug resistance for prostate cancer. Asian J Androl. 2023 Mar-Apr;25(2):208-216. doi: 10.4103/aja202281. PMID: 36412461; PMCID: PMC10069683. 11: Tan X, Ye P, Li WY, Gao Y, Leng YQ, Duan W, Wang YK, Wang WZ. The interleukin-enhanced binding factor 3-mediated inhibition of nitric oxide production via phosphoinositide 3-kinase/protein kinase B pathway contributes to central cardiovascular regulation in the rostral ventrolateral medulla in hypertension. Am J Physiol Regul Integr Comp Physiol. 2022 Dec 1;323(6):R861-R874. doi: 10.1152/ajpregu.00019.2022. Epub 2022 Oct 12. PMID: 36222883. 12: Feng D, Zhu W, You J, Shi X, Han P, Wei W, Wei Q, Yang L. Mitochondrial Aldehyde Dehydrogenase 2 Represents a Potential Biomarker of Biochemical Recurrence in Prostate Cancer Patients. Molecules. 2022 Sep 15;27(18):6000. doi: 10.3390/molecules27186000. PMID: 36144737; PMCID: PMC9500792. 13: Hossen MN, Wang L, Dwivedi SKD, Zhang Y, Rao G, Elechalwar CK, Sheth V, Dey A, Asfa S, Gulla SK, Xu C, Fung KM, Robertson JD, Bieniasz M, Wilhelm S, Bhattacharya R, Mukherjee P. Gold Nanoparticles Disrupt the IGFBP2/mTOR/PTEN Axis to Inhibit Ovarian Cancer Growth. Adv Sci (Weinh). 2022 Nov;9(31):e2200491. doi: 10.1002/advs.202200491. Epub 2022 Sep 14. PMID: 36104215; PMCID: PMC9631030. 14: Jimenez L, Amenabar C, Mayoral-Varo V, Mackenzie TA, Ramos MC, Silva A, Calissi G, Grenho I, Blanco-Aparicio C, Pastor J, Megías D, Ferreira BI, Link W. mTORC2 Is the Major Second Layer Kinase Negatively Regulating FOXO3 Activity. Molecules. 2022 Aug 24;27(17):5414. doi: 10.3390/molecules27175414. PMID: 36080182; PMCID: PMC9457944. 15: Zhang J, Li Y, Zou J, Lai CT, Zeng T, Peng J, Zou WD, Cao B, Liu D, Zhu LY, Li H, Li YK. Comprehensive analysis of the glutathione S-transferase Mu (GSTM) gene family in ovarian cancer identifies prognostic and expression significance. Front Oncol. 2022 Jul 28;12:968547. doi: 10.3389/fonc.2022.968547. PMID: 35965498; PMCID: PMC9366399. 16: Liu Z, Lin D, Zhou Y, Zhang L, Yang C, Guo B, Xia F, Li Y, Chen D, Wang C, Chen Z, Leng C, Xiao Z. Exploring synthetic lethal network for the precision treatment of clear cell renal cell carcinoma. Sci Rep. 2022 Aug 2;12(1):13222. doi: 10.1038/s41598-022-16657-7. PMID: 35918352; PMCID: PMC9345903. 17: Du C, Guan X, Yan J. Two-pore channel blockade by phosphoinositide kinase inhibitors YM201636 and PI-103 determined by a histidine residue near pore- entrance. Commun Biol. 2022 Jul 23;5(1):738. doi: 10.1038/s42003-022-03701-5. PMID: 35871252; PMCID: PMC9308409. 18: Feng D, Li D, Shi X, Xiong Q, Zhang F, Wei Q, Yang L. A gene prognostic index from cellular senescence predicting metastasis and radioresistance for prostate cancer. J Transl Med. 2022 Jun 3;20(1):252. doi: 10.1186/s12967-022-03459-8. PMID: 35658892; PMCID: PMC9164540. 19: Shi Q, Liu Y, Lu M, Lei QY, Chen Z, Wang L, He X. A pathway-guided strategy identifies a metabolic signature for prognosis prediction and precision therapy for hepatocellular carcinoma. Comput Biol Med. 2022 May;144:105376. doi: 10.1016/j.compbiomed.2022.105376. Epub 2022 Mar 9. PMID: 35286894. 20: Elmenier FM, Lasheen DS, Abouzid KAM. Design, synthesis, and biological evaluation of new thieno[2,3-d] pyrimidine derivatives as targeted therapy for PI3K with molecular modelling study. J Enzyme Inhib Med Chem. 2022 Dec;37(1):315-332. doi: 10.1080/14756366.2021.2010729. PMID: 34955086; PMCID: PMC8725920.

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