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Submit ReviewPF 04691502
Description: Potent and selective dual PI 3-K/mTOR inhibitor
Chemical Name: 2-Amino-8-[trans-4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxy-3-pyridinyl)-4-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one
Purity: ≥98% (HPLC)
Biological Activity for PF 04691502
PF 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.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for PF 04691502
PF 04691502 is also offered as part of the Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for PF 04691502
| M. Wt | 425.48 |
| Formula | C22H27N5O4 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for PF 04691502
References for PF 04691502
References are publications that support the biological activity of the product.
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
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Keywords: 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
1 Citation for PF 04691502
Citations are publications that use Tocris products. Selected citations for PF 04691502 include:
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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