WYE-354A potent, specific, and ATP-competitive inhibitor to mTOR with IC50 of 5 nM

WYE-354 (CAS 1062169-56-5)

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Synonym: 4-[6-[4-(methoxycarbonylamino)phenyl]-4-morpholin-4-ylpyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carboxylate
Application: A potent, specific, and ATP-competitive inhibitor to mTOR with IC50 of 5 nM
CAS Number: 1062169-56-5
Purity: ≥98%
Molecular Weight: 495.53
Molecular Formula: C24H29N7O5
* Refer to Certificate of Analysis for lot specific data (including water content).
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WYE-354 is an inhibitor of several PI3Ks at micromolar levels. WYE-354 is an effective inhibitor of both mTORC1 and mTORC2 in HEK293 cells. WYE-354 significantly blocks mTOR signaling and Akt activation in U87MG and MDA361 cells. WYE-354 is a potent inhibitor of proliferation in tumor cell lines including MDA-MB-361, MDA-MB-231, MDA-MB-468, LNCap, A498, and HCT116. WYE-354 induces apoptosis which is accompanied by G1 cell cycle arrest and caspases activation. WYE-354 inhibits both mTORC1 and mTORC2 signaling, as revealed by dephosphorylation of S6 ribosomal protein and Akt, respectively, in endothelial HUVEC cells. WYE-354 activates mitogen-activated protein kinase (MAPK) signaling, which may be due to its inhibition of mTORC1.

Appearance :
Crystalline
Physical State :
Solid
Solubility :
Soluble in DMSO (99 mg/mL at 25 °C), water (<1 mg/mL at 25 °C), ethanol (~0.4 mg/mL), 1:1 DMF:PBS(pH7.2) (~0.5 mg/mL), and DMF (~30 mg/mL).
Storage :
Store at -20° C
Boiling Point :
~594.2° C at 760 mmHg (Predicted)
Density :
~1.5 g/cm3 (Predicted)
Refractive Index :
n20D ~1.69 (Predicted)
IC50 :
FKBP12: IC50 = 4.3 nM (human); mTOR: IC50 = 5 nM; PI 3-kinase p110α: IC50 = 1.03 µM (human); PI3Kα: IC50 = 1.89 µM; PI3Kγ: IC50 = 7.37 µM
pK Values :
pKa: 13.42 (Predicted), pKb: 4.61 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
44219749
MDL Number :
MFCD18074514
SMILES :
COC(=O)NC1=CC=C(C=C1)C2=NC3=C(C=NN3C4CCN(CC4)C(=O)OC)C(=N2)N5CCOCC5

Download SDS (MSDS)

Certificate of Analysis

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