1. PI3K/Akt/mTOR
  2. PI3K
    mTOR

PI-103 Hydrochloride 

Cat. No.: HY-10115A Purity: 99.78%
Data Sheet SDS Handling Instructions

PI-103 hydrochloride is a potent PI3K/Akt and mTOR inhibitor with IC50 values of 2 nM for recombinant PI3K isoform p110α and 30 nM for mTOR.

For research use only. We do not sell to patients.
PI-103 Hydrochloride Chemical Structure

PI-103 Hydrochloride Chemical Structure

CAS No. : 371935-79-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
5 mg $50 In-stock
10 mg $65 In-stock
50 mg $200 In-stock
100 mg $360 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of PI-103 Hydrochloride:

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

PI-103 hydrochloride is a potent PI3K/Akt and mTOR inhibitor with IC50 values of 2 nM for recombinant PI3K isoform p110α and 30 nM for mTOR.

IC50 & Target

IC50: 30 nM (mTOR), 2 nM/3 nM/3 nM/15 nM (p110α/β/δ/γ)[1]

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].

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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.5986 mL 12.9931 mL 25.9862 mL
5 mM 0.5197 mL 2.5986 mL 5.1972 mL
10 mM 0.2599 mL 1.2993 mL 2.5986 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

Phosphatidylinositide 3-kinase inhibitory activity is determined using a scintillation proximity assay in the presence of 1 μmol/L ATP. Inhibition of mTOR protein kinase is determined using a TR-FRET-based LanthaScreen method. Compounds (PI-103) are assayed at a maximum concentration of 10 μmol/L in the presence of 1 μmol/L ATP, and IC50 values are determined[1]. 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) [3H]-thymidine. The amounts of radioactivity 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]

Mouse: 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 and/or 50 mg/kg sorafenib 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
Molecular Weight

384.82

Formula

C₁₉H₁₇ClN₄O₃

CAS No.

371935-79-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 4.1 mg/mL; H2O: < 4 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.78%

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Product Name:
PI-103 Hydrochloride
Cat. No.:
HY-10115A
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