2. PI3K/Akt/mTOR Cell Cycle/DNA Damage Autophagy Apoptosis
  3. PI3K mTOR DNA-PK Autophagy Apoptosis
  4. PI-103

PI-103 

Cat. No.: HY-10115 Purity: 98.93%
COA Handling Instructions

PI-103 est un inhibiteur puissant de PI3K et de mTOR avec des IC50 de 8 nM, 88 nM, 48 nM, 150 nM, 20 nM et 83 nM pour p110α, p110β, p110δ, p110γ, mTORC1 et mTORC2. PI-103 inhibe également DNA-PK avec une IC50 de 2 nM. PI-103 induit une autophagie.

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. PI-103 induces autophagy.

For research use only. We do not sell to patients.

PI-103 Chemical Structure

PI-103 Chemical Structure

CAS No. : 371935-74-9

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 73 In-stock
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10 mg USD 86 In-stock
50 mg USD 264 In-stock
100 mg USD 475 In-stock
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Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of PI-103:

PI-103 Related Antibodies

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mTOR mTORC1 mTORC2

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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. PI-103 induces autophagy[1][2][3][4].

IC50 & Target

p110α

8 nM (IC50)

p110β

88 nM (IC50)

p110δ

48 nM (IC50)

p110γ

150 nM (IC50)

PI3KC2β

26 nM (IC50)

PI3KC2α

1 μM (IC50)

hsVPS34

2.3 μM (IC50)

mTORC1

20 nM (IC50)

mTORC2

83 nM (IC50)

DNA-PK

2 nM (IC50)

ATR

850 nM (IC50)

ATM

920 nM (IC50)

PI4KIIIβ

50 μM (IC50)

In Vitro

PI-103 exhibits antiproliferative properties in a panel of human cancer cell lines[1]. PI-103 is essentially cytostatic for cell lines and induced cell cycle arrest in the G1 phase. In blast cells, PI-103 inhibits leukemic proliferation, the clonogenicity of leukemic progenitors and induces mitochondrial apoptosis, especially in the compartment containing leukemic stem cells [2]. PI-103 potently inhibits both the rapamycin-sensitive (mTORC1, IC50=20 nM) and rapamycin-insensitive (mTORC2, IC50=83 nM) complexes of the protein kinase mTOR[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PI-103 Related Antibodies
In Vivo

PI-103 shows therapeutic activity against a range of human tumor xenografts, exhibiting inhibition of angiogenesis, invasion, and metastasis, as well as direct antiproliferative effects[1]. PI-103 induces immunosuppression promoting in vivo tumor growth and inhibiting apoptosis. Tumors from PI-103-treated mice shows higher levels of cyclin D1 and more proliferating cells[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

348.36

Appearance

Solid

Formula

C19H16N4O3
CAS No.
SMILES

OC1=CC(C2=NC3=C(C(N4CCOCC4)=N2)OC5=C3C=CC=N5)=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (28.71 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8706 mL 14.3530 mL 28.7059 mL
5 mM 0.5741 mL 2.8706 mL 5.7412 mL
10 mM 0.2871 mL 1.4353 mL 2.8706 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.05 mg/mL (3.01 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.05 mg/mL (3.01 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 98.93%

COA (256 KB) HNMR (192 KB) LCMS (478 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[4]

IC50 values are measured using either a standard thin-layer chromatography (TLC) assay for lipid kinase activity or a high-throughput membrane capture assay. Kinase reactions are performed by preparing a reaction mixture containing kinase, inhibitor (2% DMSO final concentration), buffer (25 mM HEPES, pH 7.4, 10 mM MgCl2), and freshly sonicated phosphatidylinositol (100 μg/mL). Reactions are initiated by the addition of ATP containing 10 μCi of γ-32P-ATP to a final concentration 10 or 100 μM, and allowed to proceed for 20 minutes at room temperature. For TLC analysis, reactions are then terminated by the addition of 105 μL 1N HCl followed by 160 μL CHCl3:MeOH (1:1). The biphasic mixture is vortexed, briefly centrifuged, and the organic phase transferred to a new tube using a gel loading pipette tip precoated with CHCl3. This extract is spotted on TLC plates and developed for 3-4 hours in a 65:35 solution of n-propanol:1M acetic acid. The TLC plates are then dried, exposed to a phosphorimager screen, and quantitated. For each compound, kinase activity is typically measured at 10-12 inhibitor concentrations representing two-fold dilutions from the highest concentration tested (100 μM). For compounds showing significant activity, IC50 determinations are repeated two to four times, and the reported value is the average of these independent measurements[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

For proliferation assays, MOLM14, OCI-AmL3 and MV4-11 cells are cultured during 48 h at 105 cells/mL, in triplicate, in 10% FCS, without or with 0.1 or 1 μM PI-103, and then pulsed 6 h with 1μCi (37 kBq) [4H]-thymidine. The amounts oadioactivity are determined after trichloracetic acid precipitation[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Mice[3]
Five to six month old males of either FVB/N strain or nude BALB/c strain are injected subcutaneously with one million cells in PBS. When tumor reaches between 50 and 100 mm3, mice are treated with 10 mg/kg or 70 mg/kg of PI-103 by IP injection daily. Control mice are treated with the same volume of DMSO. Tumor size and mice weight is monitored every 2 days. When mice are sacrificed, tumors are dissected and processed[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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PI-103 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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The dilution calculator equation

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Keywords:

PI-103371935-74-9PI103PI 103PI3KmTORDNA-PKAutophagyApoptosisPhosphoinositide 3-kinaseMammalian target of RapamycinDNA-dependent protein kinaseInhibitorinhibitorinhibit

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