PI-103 hydrochloride

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 hydrochloride | PI103 hydrochloride

PI3K/Akt/mTOR signaling

PI3K

PI3K

Cancer

——

371935-79-4

384.8163

C19H17ClN4O3

>98% (HPLC)

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

C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O.Cl

Phenol, 3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years