WYE-125132 Inhibitor CAS No. 1144068-46-1

Cat. No.	Name	Size	Price
KI1444	WYE-125132	5 mg	$310
	WYE-125132	10 mg	$592
	WYE-125132	50 mg	$1512
	WYE-125132	100 mg	$2700

Chemical Characteristic

Product Name	WYE-125132
CAS No.	1144068-46-1
Molecular Weight	519.6
Formula	C₂₇H₃₃N₇O₄
Chemical Name	Urea, N-[4-[1-(1,4-dioxaspiro[4.5]dec-8-yl)-4-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-N'-methyl-
Smiles	N(C(=O)NC)c1ccc(cc1)c1nc2c(c(n1)N1CC3CCC(C1)O3)cnn2C1CCC2(OCCO2)CC1
Chemical Structure

Biological activities

WYE-125132 is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor. The IC50 value of WYE-125132 is 0.19 nM against mTOR. Consistent with genetic ablation of mTORC2, WYE-125132 targets P-AKT(S473) and AKT function without significantly reducing the steady-state level of the PI3K/PDK1 activity biomarker P-AKT(T308) in cancer cells. Compared with the rapalog temsirolimus/CCI-779, WYE-125132 elicits a substantially stronger inhibition of cancer cell growth and survival, protein synthesis, cell size, bioenergetic metabolism, and adaptation to hypoxia in vitro.^[1] In vitro, WYE-125132 treatment also leads to a rapid loss of the phosphorylation at Ser-75 of Maf1.^[2] In tumor-bearing mice, oral administration of WYE-125132 has potent single-agent antitumor activity against MDA361 breast, U87MG glioma, A549 and H1975 lung, as well as A498 and 786-O renal tumors. When coadministered with bevacizumab, WYE-125132 achieves a substantial regression of MDA361 and A549 large tumors and causes complete regression of A498 large tumors.^[1]

Protocols

WYE-125132 is dissolved in DMSO.^[2]

References

[1] Yu K, et al. Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2. Cancer Res. 2010, 70(2): 621-631. [2] Shor B, et al. Requirement of the mTOR kinase for the regulation of Maf1 phosphorylation and control of RNA polymerase III-dependent transcription in cancer cells. J Biol Chem. 2010, 285(20): 15380-15392.

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