WYE-354

WYE-354

Catalog Number:
L002368291APE
Mfr. No.:
APE-A1266
Price:
$254
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      • Overview
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          Background

          WYE-354 is a powerful and selective ATP-competitive kinase heterocyclic inhibitors with biochemical IC50 of 5 nM against mTOR.[1]WYE-354 displays very specific selectivity to PI3K families (>100-fold to PI3K and >500-fold to PI3K), but it can’t inhibit some protein kinases. May cancer cell lines including MDA-MB-468 and U87MG can be inhibited by WYE-354 in 0.3–1 mM range.[1]In-vitro study has proved that WYE-354 can inhibit substrate phosphorylation such as p-4E-BP1 T37/46 and p-Akt S473 by mTORC1 and mTORC2. WYE-354 can reduce Akt downstream function and block the propagation of the cancer cell lines with an IC50 value from sub-micromolar to micromolar range [3]. These effects were consistent with the G1 cell cycle arrest in two cell lines, including rapamycin-sensitive and rapamycin-resistant cells. It is believed to induce apoptosis, repress the global protein synthesis, and down-regulate many angiogenic factors.[3]

          [1] Qingsong Liu, Carson Thoreen, Jinhua Wang, David Sabatini, Nathanael S. Gray. mTOR mediated anti-cancer drug discovery. Drug Discovery Today. 2009. 6(2): 47-55.
          [2] Shi-Yong Sun. mTOR kinase inhibitors as potential cancer therapeutic drugs. Cancer Letters. 28 October 2013. 340(1): 1-8.

      • Properties
        • Alternative Name
          methyl 4-[6-[4-(methoxycarbonylamino)phenyl]-4-morpholin-4-ylpyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carboxylate
          CAS Number
          1062169-56-5
          Molecular Formula
          C24H29N7O5
          Molecular Weight
          495.53
          Appearance
          A solid
          Purity
          98.06%
          Solubility
          ≥49.6 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
          Storage
          Store at -20°C

          * For Research Use Only

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