WYE-687
WYE-687 is an ATP-competitive inhibitor of mTOR with IC50 value of 7nM [1].
WYE-687 is a small-molecule pyrazolopyrimidine inhibitor of mTOR1 and mTOR2. In the immune-complex kinase assay using His6-AKT and His6-S6K as the specific substrates of mTOR1 and mTOR2, WYE-687 prevents mTOR from phosphorylating the substrates dose-dependently. Besides that, WYE-687 is found to highly selective against PI3Kα (>100-fold) and PI3Kγ (>500-fold) as well as 24 other protein kinases. It is found that WYE-687 can suppress cell growth via causing a strong G1 arrest in cell cycle in tumor cell lines including MDA361 and HCT116. WYE-687 also affects the angiogenic factor of cancer cells. It reduces the expression of HIF-1α in U87MG, MDA361 and LNCap cells [1].
References:
[1] Yu K, Toral-Barza L, Shi C, et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer research, 2009, 69(15): 6232-6240.
| Storage | Store at -20°C |
| M.Wt | 528.61 |
| Cas No. | 1062161-90-3 |
| Formula | C28H32N8O3 |
| Solubility | insoluble in H2O; insoluble in EtOH; insoluble in DMSO |
| Chemical Name | methyl N-[4-[4-morpholin-4-yl-1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]carbamate |
| SDF | Download SDF |
| Canonical SMILES | COC(=O)NC1=CC=C(C=C1)C2=NC3=C(C=NN3C4CCN(CC4)CC5=CN=CC=C5)C(=N2)N6CCOCC6 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | WYE-687 is an ATP-competitive and selective inhibitor of mTOR with an IC50 value of 7 nM. | |||||
| Targets | mTOR | PI3Kα | PI3Kγ | p38α | Src | |
| IC50 | 7 nM | 0.81 μM | 3.11 μM | 28.9μM | >50 μM | |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
