ChemicalBook > CAS DataBase List > WYE-354

WYE-354

Product Name
WYE-354
CAS No.
1062169-56-5
Chemical Name
WYE-354
Synonyms
CS-441;WYE-354;Wye354 Wye-354;WYE-354 USP/EP/BP;WYE-354 (Degrasyn);WYE-354, 10 mM in DMSO;WYE-354;WYE 354; WYE354;mTOR Kinase Inhibitor II WYE-354 WYE354;Methyl 4-(6-(4-(methoxycarbonylamino)phenyl)-4-morpholino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pip;methyl 4-[6-[4-(methoxycarbonylamino)phenyl]-4-morpholin-4-ylpyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carboxylate
CBNumber
CB92512520
Molecular Formula
C24H29N7O5
Formula Weight
495.53
MOL File
1062169-56-5.mol
More
Less

WYE-354 Property

Density 
1.46
storage temp. 
Sealed in dry,Store in freezer, under -20°C
solubility 
≥49.6 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
form 
solid
pka
13.42±0.70(Predicted)
color 
White to off-white
InChIKey
IMXHGCRIEAKIBU-UHFFFAOYSA-N
SMILES
N1(C(OC)=O)CCC(N2C3C(C=N2)=C(N2CCOCC2)N=C(C2=CC=C(NC(OC)=O)C=C2)N=3)CC1
More
Less

Hazard and Precautionary Statements (GHS)

More
Less

N-Bromosuccinimide Price

Sigma-Aldrich
Product number
475986
Product name
mTOR Kinase Inhibitor II, WYE-354 - CAS 1062169-56-5 - Calbiochem
Packaging
5MG
Price
$278
Updated
2025/07/31
Cayman Chemical
Product number
13604
Product name
WYE-354
Purity
≥98%
Packaging
5mg
Price
$93
Updated
2024/03/01
Cayman Chemical
Product number
13604
Product name
WYE-354
Purity
≥98%
Packaging
10mg
Price
$176
Updated
2024/03/01
Cayman Chemical
Product number
13604
Product name
WYE-354
Purity
≥98%
Packaging
25mg
Price
$412
Updated
2024/03/01
Cayman Chemical
Product number
13604
Product name
WYE-354
Purity
≥98%
Packaging
50mg
Price
$728
Updated
2024/03/01
More
Less

WYE-354 Chemical Properties,Usage,Production

Description

WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2. It is a much weaker inhibitor of phosphatidylinositol 3-kinase α (IC50 = 1,026 nM) and other kinases. WYE-354 induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines, inhibits mTORC1 and mTORC2 in tumor-bearing mice, and reduces tumor growth in nude mice with PTEN-null tumors.

Uses

A pyrazolopyrimidines derivative that is a potent and ATP-competitive mTOR inhibitor with much reduced activity against PI 3-Kα or PI 3-Kγ. WYE-354 is equally potent against mTORC1 and mTORC2 activities in HEK293 immune complex kinase assays using S6K and Akt as the respective substrate (IC50 <200 nM; [ATP] = 100 μM) and effectively blocks cellular phosphorylation of S6K on T389 and Akt on S473 both in cultures and in a murine xenograft model, resulting in a significant suppression of PC3MM2-derived tumor growth (by 86% on day 7; 50 mg/kg, i.p twice per day) in vivo.

Definition

ChEBI: 4-[6-[4-(methoxycarbonylamino)phenyl]-4-(4-morpholinyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinecarboxylic acid methyl ester is a carbamate ester.

in vivo

The effect of Rapamycin and WYE-354 on tumor growth is evaluated in xenograft GBC tumor models. 2×106 or 5×106 cells of G-415 or TGBC2TKB, respectively, are xenotransplanted into NOD-SCID mice subcutaneously. When tumors reach an average volume of 100 mm3, the mice are treated either with Rapamycin or WYE354. Rapamycin is administered i.p. at a concentration of 10 mg/kg, daily for 5 days per week for 3 weeks, while WYE-354 is administrated at a daily i.p. dose of 50 mg/kg for 5 days. Mice are sacrificed 30 days after the initiation of the treatments and an autopsy is performed that include removal of the entire tumor area. Mice treated with WYE-354 exhibit 68.6% and 52.4% reduction in average tumor size (P<0.01; P<0.01), as well as 82.9% and 45.5% (P<0.01; ns) reduction in tumor weight, respectively[2].

target

mTOR

IC 50

mTOR: 5 nM (IC50); mTORC1; mTORC2; PI3K alpha: 1.89 μM (IC50); PI3K gamma: 7.37 μM (IC50); Autophagy

References

[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.

WYE-354 Preparation Products And Raw materials

Raw materials

Preparation Products

More
Less

WYE-354 Suppliers

Canada 1 China 105 France 1 India 1 United States 14 Global 122
Alsachim SAS
Tel
--
Fax
--
Email
sales@alsachim.com
Country
France
ProdList
424
Advantage
0
More
Less

View Lastest Price from WYE-354 manufacturers

Career Henan Chemical Co
Product
WYE-354 1062169-56-5
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
ask
Release date
2018-12-23

1062169-56-5, WYE-354Related Search:

WYE 354-d3 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'-methylurea WYE-687 Selumetinib U0126-EtOH MK-2206 2HCl 1,9-Pyrazoloanthrone KU-0063794 BEZ235 (NVP-BEZ235, Dactolisib)

  • WYE-354
  • 4-[6-[4-[(Methoxycarbonyl)amino]phenyl]-4-(4-morpholinyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinecarboxylic acid methyl ester
  • methyl 4-[6-[4-(methoxycarbonylamino)phenyl]-4-morpholin-4-ylpyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carboxylate
  • WYE-354 (Degrasyn)
  • WYE-354;WYE 354; WYE354
  • CS-441
  • Methyl 4-(6-(4-(methoxycarbonylamino)phenyl)-4-morpholino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pip
  • 1-Piperidinecarboxylic acid, 4-[6-[4-[(methoxycarbonyl)amino]phenyl]-4-(4-morpholinyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-, methyl ester
  • WYE-354 USP/EP/BP
  • Methyl 4-(6-(4-((methoxycarbonyl)amino)phenyl)-4-morpholino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate
  • mTOR Kinase Inhibitor II WYE-354 WYE354
  • Wye354 Wye-354
  • WYE-354, 10 mM in DMSO
  • 1062169-56-5
  • C24H29N7O5
  • Amines
  • Aromatics
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Protein Kinase Inhibitors and Activators
  • PI3K/Akt/mTOR
  • Inhibitors
  • Akt
  • mTOR
  • PI3K