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

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.

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PI-103 構造式

PI-103 構造式

CAS 番号 : 371935-74-9

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 在庫あり
Solution
10 mM * 1 mL in DMSO USD 73 在庫あり
Solid
5 mg USD 66 在庫あり
10 mg USD 86 在庫あり
50 mg USD 264 在庫あり
100 mg USD 475 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 20 publication(s) in Google Scholar

Other Forms of PI-103:

PI-103 関連抗体

Top Publications Citing Use of Products

PI3K アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

mTOR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
mTOR mTORC1 mTORC2

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

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)

体外実験

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 関連抗体
体内実験

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.
分子量

348.36

分子式

C19H16N4O3
CAS 番号
Appearance

Solid

Color

Light yellow to green yellow

SMILES

OC1=CC(C2=NC3=C(C(N4CCOCC4)=N2)OC5=C3C=CC=N5)=CC=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 10 mg/mL (28.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 1.05 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

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

    This protocol yields a clear solution of ≥ 1.05 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 98.93%

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

取扱説明書 (2659 KB)
参考文献
キナーゼ実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
細胞実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
動物実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8706 mL 14.3530 mL 28.7059 mL 71.7648 mL
5 mM 0.5741 mL 2.8706 mL 5.7412 mL 14.3530 mL
10 mM 0.2871 mL 1.4353 mL 2.8706 mL 7.1765 mL
15 mM 0.1914 mL 0.9569 mL 1.9137 mL 4.7843 mL
20 mM 0.1435 mL 0.7176 mL 1.4353 mL 3.5882 mL
25 mM 0.1148 mL 0.5741 mL 1.1482 mL 2.8706 mL
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PI-103 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

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

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