PI-103

Research use only, not for human use.

A potent, dual class I PI3K/mTOR inhibitor with IC50 of 2/3/3/15/ for p110α/β/δ/γ, respectively.

A potent, dual class I PI3K/mTOR inhibitor with IC50 of 2/3/3/15/ for p110α/β/δ/γ, respectively; also inhibits TORC1 (>80% inhibition at 0.5 uM) and DNA-PK (IC50=14 nM), 15- to 20-fold less activity against class II PI3K C2β (IC50=43 nM), >1,300-fold selectivity over the class III PI3K Vsp34; potently inhibits proliferation and invasion of a wide variety of human cancer cells in vitro; shows activity in cancer xenograft models.

PI-103 exhibits antiproliferative properties in a panel of human cancer cell lines. 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 . 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.

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. 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.

PI 103 | PI103

PI3K/Akt/mTOR signaling

PI3K

DNA-PK|p110α|p110β|p110γ|p110δ|mTOR

Cancer

——

371935-74-9

348.3553

C19H16N4O3

>98% (HPLC)

10 mM in DMSO

OC1=CC(=CC=C1)C1=NC2=C(OC3=C2C=CC=N3)C(=N1)N1CCOCC1 |c:3,5,13,16,18,21,t:1,8,10|

Phenol, 3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]-

(-20℃)

With Ice Pack

≥ 2 years