WYE-125132
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MedKoo CAT#: 406366

CAS#: 1144068-46-1

Description: WYE-125132, also known as WYE-132, is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor (IC(50): 0.19 +/- 0.07 nmol/L; >5,000-fold selective versus PI3Ks). WYE-132 inhibited mTORC1 and mTORC2 in diverse cancer models in vitro and in vivo. Importantly, consistent with genetic ablation of mTORC2, WYE-132 targeted P-AKT(S473) and AKT function without significantly reducing the steady-state level of the PI3K/PDK1 activity biomarker P-AKT(T308), highlighting a prominent and direct regulation of AKT by mTORC2 in cancer cells.


Price and Availability

Size
Price

2mg
USD 90
Size
Price

5mg
USD 150
Size
Price

10mg
USD 250

WYE-125132, purity > 98%, is in stock. The same day shipping out after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Note: the estimated shipping out time for order > 10mg may be 2 months


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406366
Name: WYE-125132
CAS#: 1144068-46-1
Chemical Formula: C27H33N7O4
Exact Mass: 519.2594
Molecular Weight: 519.6
Elemental Analysis: C, 62.41; H, 6.40; N, 18.87; O, 12.32


Synonym: WYE 125132, WYE-125132, WYE125132, WYE132, WYE 132, WYE-132

IUPAC/Chemical Name: 1-(4-(4-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)-1-(1,4-dioxaspiro[4.5]decan-8-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl)-3-methylurea

InChi Key: QLHHRYZMBGPBJG-UHFFFAOYSA-N

InChi Code: InChI=1S/C27H33N7O4/c1-28-26(35)30-18-4-2-17(3-5-18)23-31-24(33-15-20-6-7-21(16-33)38-20)22-14-29-34(25(22)32-23)19-8-10-27(11-9-19)36-12-13-37-27/h2-5,14,19-21H,6-13,15-16H2,1H3,(H2,28,30,35)

SMILES Code: O=C(NC)NC1=CC=C(C2=NC(N3CC(O4)CCC4C3)=C5C(N(C(CC6)CCC76OCCO7)N=C5)=N2)C=C1


Technical Data

Appearance:
White solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Yu K, Toral-Barza L. Biochemical and pharmacological inhibition of mTOR by rapamycin and an ATP-competitive mTOR inhibitor. Methods Mol Biol. 2012;821:15-28. doi: 10.1007/978-1-61779-430-8_2. PubMed PMID: 22125057.

2: Shor B, Wu J, Shakey Q, Toral-Barza L, Shi C, Follettie M, Yu K. 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 May 14;285(20):15380-92. doi: 10.1074/jbc.M109.071639. Epub 2010 Mar 16. PubMed PMID: 20233713; PubMed Central PMCID: PMC2865278.

3: Yu K, Shi C, Toral-Barza L, Lucas J, Shor B, Kim JE, Zhang WG, Mahoney R, Gaydos C, Tardio L, Kim SK, Conant R, Curran K, Kaplan J, Verheijen J, Ayral-Kaloustian S, Mansour TS, Abraham RT, Zask A, Gibbons JJ. Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2. Cancer Res. 2010 Jan 15;70(2):621-31. doi: 10.1158/0008-5472.CAN-09-2340. Epub 2010 Jan 12. PubMed PMID: 20068177.