Other drug agents
MedKoo product information:
Description of PF-04691502: PF-04691502 is a PI3K/mTOR kinase inhibitor, 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. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
Current developer: Pfizer
an ATP-competitive PI3K/mTOR dual inhibitor, which potently inhibited
recombinant class I PI3K and mTOR in biochemical assays and suppressed
transformation of avian fibroblasts mediated by wild-type PI3K γ, δ, or
mutant PI3Kα. In PIK3CA-mutant and PTEN-deleted cancer cell lines,
reduced phosphorylation of AKT T308 and AKT S473 (IC(50) of 7.5-47 nmol/L
and 3.8-20 nmol/L, respectively) and inhibited cell proliferation
(IC(50) of 179-313 nmol/L).
inhibited mTORC1 activity in cells as measured by PI3K-independent
nutrient stimulated assay, with an IC(50) of 32 nmol/L and inhibited the
activation of PI3K and mTOR downstream effectors including AKT, FKHRL1,
PRAS40, p70S6K, 4EBP1, and S6RP. Short-term exposure to
predominantly inhibited PI3K, whereas mTOR inhibition persisted for 24
to 48 hours.
PF-04691502 induced cell cycle G(1) arrest, concomitant with
upregulation of p27 Kip1 and reduction of Rb. Antitumor activity was
observed in U87 (PTEN null), SKOV3 (PIK3CA mutation), and gefitinib- and
erlotinib-resistant non-small cell lung carcinoma xenografts. In
is a potent dual PI3K/mTOR inhibitor with broad antitumor activity.
entered phase I clinical trials. (source:
Mol Cancer Ther. 2011 Nov;10(11):2189-99).
(source: Mol Cancer Ther. 2011 Nov;10(11):2189-99).
1. Highly Selective and Potent Thiophenes as PI3K
Inhibitors with Oral Antitumor Activity [Erratum to document cited in
CA155:552621] By Liu, Kevin K.-C.; Zhu, Jin Jiang; Smith, Graham L.;
Yin, Min-Jean; Bailey, Simon; Chen, Jeffrey H.; Hu, Qiyue; Huang, Qinhua;
Li, Chunze; Li, Qing J.; et al From ACS Medicinal Chemistry Letters,
Ahead of Print.
(Keyword; CAS#; MedKoo code#)
About us | Services | Products | News | Careers | Contact us