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Submit ReviewPF 04691502 is a potent and selective dual ATP-competitive PI 3-K/mTOR inhibitor (Ki values are 1.6, 1.8, 1.9, 2.1 and 16 nM for human PI 3-K δ, α, γ, β, and mTOR, respectively). Displays no significant inhibitory activity at more than 80 protein kinases (concentration ≥ 10 μM) including hVps34, PI 3-K downstream kinases, and MAPK family members. Orally bioavailable. Induces robust cell cycle arrest at the G1 phase in U87MG cancer cells and antitumor activity in SKOV3 ovarian cancer xenograft models.
Sold for research purposes under agreement from Pfizer Inc.
PF 04691502 is also offered as part of the Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 425.48 |
公式 | C22H27N5O4 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1013101-36-4 |
PubChem ID | 25033539 |
InChI Key | XDLYKKIQACFMJG-UHFFFAOYSA-N |
Smiles | O=C2C(C4=CC=C(OC)N=C4)=CC1=C(C)N=C(N)N=C1N2[C@@H]3CC[C@@H](OCCO)CC3 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Yuan et al (2011) PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity. Mol.Cancer Ther. 10 2189 PMID: 21750219
关键词: PF 04691502, PF 04691502 supplier, PF04691502, phosphoinositide, 3-kinases, PI, 3-K/mTOR, mammalian, Target, Rapamycin, FRAP, FK506, binding, protein, 12, FKBP12, rapamycin, associated, cell, cycle, antitumor, 3-Kinase, mTOR, 4820, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PF 04691502 的部分引用包括:
Carsten et al (2017) Combined inhibition of GLI and FLT3 signaling leads to effective anti-leukemic effects in human acute myeloid leukemia. Oncotarget 8 29187-29201 PMID: 28418873
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