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Products are for research use only. Not for human use. We do not sell to patients.
(PF 04691502; PF04691502)
PF-04691502 Chemical Structure
|Product name: PF-04691502|
|Cat. No.: HY-15177|
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)
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.
|M.Wt||425.48||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.3503 mL||11.7514 mL||23.5029 mL|
|5 mM||0.4701 mL||2.3503 mL||4.7006 mL|
|10 mM||0.2350 mL||1.1751 mL||2.3503 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|PF-04691502||Pfizer Inc||Metastatic breast cancer||31-JAN-13||30-APR-15||Phase 2||11-SEP-13|
|Pfizer Inc||Advanced solid tumor||31-DEC-09||30-APR-12||Phase 1||31-MAY-12|
|Pfizer Inc||Endometrioid carcinoma||01-JAN-12||31-MAY-14||Phase 2||28-NOV-13|
|Pfizer Inc||Breast tumor||31-MAR-12||31-DEC-12||Phase 2||26-DEC-12|
|Pfizer Inc||Advanced solid tumor||31-OCT-11||30-NOV-14||Phase 1||06-NOV-13|
. Kinross KM, Brown DV, Kleinschmidt M et al. In vivo activity of combined PI3K/mTOR and MEK inhibition in a Kras(G12D);Pten deletion mouse model of ovarian cancer. Mol Cancer Ther. 2011 Aug;10(8):1440-9.
. Simmons BH, Lee JH, Lalwani Ket al. Combination of a MEK inhibitor at sub-MTD with a PI3K/mTOR inhibitor significantly suppresses growth of lung adenocarcinoma tumors in Kras(G12D-LSL) mice. Cancer Chemother Pharmacol. 2012 Aug;70(2):213-20.
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