PI-103 free base · Synonyms: PI 103 · PI103

PI-103 is a potent PI3K and mTOR inhibitor.

For research use only. Not for human or veterinary use.

Target PI3K mTOR DNA-PK Autophagy Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

PI-103 structure

CAS No.: 371935-74-9

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 550.00	BP-02119-250mg	In stock	Get quote
500 mg	USD 780.00	BP-02119-50mg	In stock	Get quote
1 g	USD 1,250.00	BP-02119-1g	In stock	Get quote
2 g	USD 1,950.00	BP-02119-2g	In stock	Get quote
5 g	USD 3,650.00	BP-02119-5g	In stock	Get quote

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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 .

Biological activity

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. 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.

Identifiers

SMILES: OC1=CC=CC(=C1)C1=NC(N2CCOCC2)=C2OC3=NC=CC=C3C2=N1
InChIKey: TUVCWJQQGGETHL-UHFFFAOYSA-N

Specifications

MW (average): 348.3553
Formula: C₁₉H₁₆N₄O₃
CAS No.: 371935-74-9
Physical state: Solid
Color: Off-white to light green
Shipping: 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: Powder -20℃ 3 years; 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Raynaud FI, et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103through PI-540, PI-620 to the oral agent GDC-0941. Mol Cancer Ther. 2009 Jul;8(7):1725-39.

[2]. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110 alpha. Cell. 2006 May 19;125(4):733-47.

[3]. Park S, et al. PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase anLeukemia. 2008 Sep;22(9):1698-706.d mTOR, has antileukemicactivity in AmL. Leukemia. 2008 Sep;22(9):1698-706.

[4]. López-Fauqued M, et al. The dual PI3K/mTOR inhibitor PI-103 promotes immunosuppression, in vivo tumor growth and increases survival of melanoma cells. Int J Cancer. 2010 Apr 1;126(7):1549-61.

Same target

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Same research area

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