Brief Description

PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK.
IC50 value: 1.8 nM/2.1 nM/1.6 nM/1.9 nM(PI3Kα/β/δ/γ); 16 nM(mTOR)
Target: PI3K/mTOR
PF-04691502 is an ATP-competitive PI3K/mTOR dual inhibitor with IC50 of 32 nM. PF-04691502 is also an agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. PI3K/mTOR kinase inhibitor PF-04691502 inhibits both PI3K and mTOR kinases, which may result in apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K. PF-04691502 is currently in Phase II clinical trials in patients with recurrent endometrial cancer and Breast Cancer. A Phase II clinical trials in patients with solid tumors has been completed.

Solubility

DMSO > 60 mg/mL; Ethanol > 60 mg/mL

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

white to gray solid