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Chemical Structure| 371935-74-9 Chemical Structure| 371935-74-9

Structure of PI-103
CAS No.: 371935-74-9

Chemical Structure| 371935-74-9

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PI-103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. It blocks autophagic flux.

Synonyms: PI-103

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Product Details of PI-103

CAS No. :371935-74-9
Formula : C19H16N4O3
M.W : 348.36
SMILES Code : OC1=CC=CC(C2=NC(N3CCOCC3)=C(OC4=NC=CC=C45)C5=N2)=C1
Synonyms :
PI-103
MDL No. :MFCD11983145

Safety of PI-103

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P261-P305+P351+P338

Related Pathways of PI-103

DNA
PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110γ

    p110γ, IC50:15 nM

  • p110β

    p110β, IC50:3 nM

  • p110α

    p110α, IC50:2 nM

  • p110δ

    p110δ, IC50:3 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
LNCaP cells 3 μM PI-103 significantly reduced CXCL13-mediated migration and invasion of LNCaP cells, indicating that LNCaP cell migration and invasion are dependent on PI3Kp110α. PMC2873439
PC3 cells 3 μM PI-103 significantly reduced CXCL13-mediated migration and invasion of PC3 cells, indicating that PC3 cell migration and invasion are dependent on PI3Kp110α. PMC2873439
4T1 breast cancer cells 5 μM 48 h Evaluate the effect of PI103 and PI103-SNP on the viability of 4T1 cells, results show that PI103-SNP sustained inhibition of Akt phosphorylation PMC3855341
MDA-MB-468 breast cancer cells 5 μM 48 h Evaluate the effect of PI103 and PI103-SNP on the viability of MDA-MB-468 cells, results show that PI103-SNP sustained inhibition of Akt phosphorylation PMC3855341
4306 ovarian cancer cells 5 μM 48 h Evaluate the effect of PI103 and PI103-SNP on the viability of 4306 cells, results show that PI103-SNP sustained inhibition of Akt phosphorylation PMC3855341
HCT116 BAX-ko cells 20 μM 24 h Induced autophagy, increased de novo ChoPL synthesis PMC7469489
HT29 cells 100 μM 24 h Induced autophagy, increased de novo ChoPL synthesis PMC7469489
16HBE cells 10 ng/ml 24 h To investigate the effect of PI-103 on IL-13-induced ER stress and mucus overproduction, results showed that PI-103 significantly reduced the fluorescence intensities of BIP and CHOP and decreased MUC5AC expression. PMC5233819
MDA-MB-231 50 µM 72 h To assess the toxicity effect of RIDR-PI-103 on breast cancer cells, results showed that MDA-MB-231 cells were sensitive to RIDR-PI-103. PMC7923228
MDA-MB-361 50 µM 72 h To assess the toxicity effect of RIDR-PI-103 on breast cancer cells, results showed that MDA-MB-361 cells were sensitive to RIDR-PI-103. PMC7923228
MDA-MB-453 50 µM 72 h To assess the toxicity effect of RIDR-PI-103 on breast cancer cells, results showed that MDA-MB-453 cells were sensitive to RIDR-PI-103. PMC7923228

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice PDX model intraperitoneal injection 10 mg/kg daily for 3 weeks To investigate the inhibitory effect of PI-103 on tumor growth in the PDX model, it was found that PI-103 significantly reduced the tumor burden. PMC7471427
Mice 4T1 breast cancer model Tail vein injection 5 mg/kg Every 48 hours for 3 doses Evaluate the antitumor efficacy of PI103-SNP in the 4T1 breast cancer model, results show that PI103-SNP significantly inhibited tumor growth and prolonged survival PMC3855341
C57BL/6J mice C57BL/6J mice Intraperitoneal injection 20 mg/kg Single dose, duration of 96 hours To evaluate the pharmacokinetic profile of RIDR-PI-103 in mice, results showed that the maximum plasma concentration of RIDR-PI-103 was 201.5 ng/mL with a half-life of 9.4 hours. PMC7923228

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.87mL

0.57mL

0.29mL

14.35mL

2.87mL

1.44mL

28.71mL

5.74mL

2.87mL

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