ChemicalBook > CAS DataBase List > WYE-687

WYE-687

Product Name
WYE-687
CAS No.
1062161-90-3
Chemical Name
WYE-687
Synonyms
CS-540;WYE-687;1?N, 97%);L-Leucine-d;WYE-687 WYE687;WYE-687 USP/EP/BP;WYE-687;WYE 687;WYE687;WYE-687, 10 mM in DMSO;17α-Ethynyltestosterone;4-Oxo-2,2,6,6-tetramethylpiperidine (tempone precursor) (D??, 97%
CBNumber
CB12561502
Molecular Formula
C28H32N8O3
Formula Weight
528.61
MOL File
1062161-90-3.mol
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WYE-687 Property

Density 
1.40
storage temp. 
Store at -20°C
solubility 
insoluble in H2O; insoluble in EtOH; insoluble in DMSO
form 
Powder
pka
13.42±0.70(Predicted)
color 
Off-white to yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML3375
Product name
WYE-687
Purity
≥98% (HPLC)
Packaging
5MG
Price
$79.32
Updated
2025/07/31
Sigma-Aldrich
Product number
SML3375
Product name
WYE-687
Purity
≥98% (HPLC)
Packaging
25MG
Price
$336
Updated
2025/07/31
Cayman Chemical
Product number
29977
Product name
WYE-687
Packaging
1mg
Price
$48
Updated
2024/03/01
Cayman Chemical
Product number
29977
Product name
WYE-687
Packaging
25mg
Price
$636
Updated
2024/03/01
Cayman Chemical
Product number
29977
Product name
WYE-687
Packaging
5mg
Price
$152
Updated
2024/03/01
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WYE-687 Chemical Properties,Usage,Production

Uses

WYE-687 is an ATP-competitive and selective inhibitor of mammalian target of rapamycin (mTOR). Studies have shown the combination of Ras-Raf-MEK1/2 inhibitors with WYE-687 may overcome resistance to mTorKIs thus may be an effective additive therapy for treatment of patient with renal cell carcinoma or colorectal cancer.

Biological Activity

wye-687 is an atp-competitive inhibitor of mtor with ic50 value of 7nm [1].wye-687 is a small-molecule pyrazolopyrimidine inhibitor of mtor1 and mtor2. in the immune-complex kinase assay using his6-akt and his6-s6k as the specific substrates of mtor1 and mtor2, wye-687 prevents mtor from phosphorylating the substrates dose-dependently. besides that, wye-687 is found to highly selective against pi3kα (>100-fold) and pi3kγ (>500-fold) as well as 24 other protein kinases. it is found that wye-687 can suppress cell growth via causing a strong g1 arrest in cell cycle in tumor cell lines including mda361 and hct116. wye-687 also affects the angiogenic factor of cancer cells. it reduces the expression of hif-1α in u87mg, mda361 and lncap cells [1].

in vivo

U937 cells are inoculated into the flanks of SCID/beige mice. When xenografted tumors reach a volume around 100 mm3, mice are orally administrated with either vehicle control (5% ethanol, 2% Tween 80, and 5% polyethylene glycol-400) or WYE-687 (5 or 25 mg/kg) daily for a total of 7 days. The WYE-687 regimen utilized in this study is based on preexperimental results and related studies. WYE-687 administration (5 or 25 mg/kg, daily) significantly inhibits U937 xenograft tumor growth in SCID mice, and the in vivo activity by WYE-687 is dose-dependent. At day 15, the 5 mg/kg WYE-687-treated tumors and 25 mg/kg WYE-687-treated tumors are 50% and 75% smaller than the vehicle control tumors, respectively. Tumor weights of WYE-687-treated mice are also significantly lower than that of vehicle group. Oral administration of WYE-687 potently inhibits U937 leukemic xenograft tumor growth in SCID mice, without causing significant toxicities[2].

IC 50

mTOR: 7 nM (IC50); mTORC1; mTORC2; PI3K alpha: 81 nM (IC50); PI3K gamma: 3.11 μM (IC50); CK1 gamma1: 17.8 μM (IC50); p38 alpha: 28.9 μM (IC50)

References

[1] yu k, toral-barza l, shi c, et al. biochemical, cellular, and in vivo activity of novel atp-competitive and selective inhibitors of the mammalian target of rapamycin. cancer research, 2009, 69(15): 6232-6240.

WYE-687 Preparation Products And Raw materials

Raw materials

Preparation Products

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WYE-687 Suppliers

Canada 1 China 99 India 1 United Kingdom 1 United States 14 Global 116
J & K SCIENTIFIC LTD.
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18210857532; 18210857532
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Chembest Research Laboratories Limited
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+86-21-20908456
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Jinan Trio PharmaTech Co., Ltd.
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Hunan Hui Bai Shi Biotechnology Co., Ltd.
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0731-85526065 13308475853
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NCE Biomedical Co.,Ltd.
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Shanghai Aladdin Bio-Chem Technology Co.,LTD
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AdooQ BioScience, LLC
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ShangHai Caerulum Pharma Discovery Co., Ltd.
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18149758185
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Suzhou yacoo science co.,Ltd
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1062161-90-3, WYE-687Related 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-354 MK-2206 2HCl CX-4945 PaloMid 529 (P529) Trametinib GSK429286A Rapamycin

  • methyl 4-(4-morpholino-1-(1-(pyridin-3-ylmethyl)piperidin-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-yl)phenylcarbamate
  • methyl N-[4-[4-morpholin-4-yl-1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]carbamate
  • WYE-687;WYE 687;WYE687
  • WYE-687
  • N-[4-[4-(4-Morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]carbamic acid methyl ester
  • N-[4-[4-(4-Morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-carbamic acid methyl ester hydrochloride
  • CS-540
  • Carbamic acid, N-[4-[4-(4-morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-, methyl ester
  • WYE-687 USP/EP/BP
  • 17α-Ethynyltestosterone
  • WYE-687 WYE687
  • L-Leucine-d
  • WYE-687, 10 mM in DMSO
  • 4-Oxo-2,2,6,6-tetramethylpiperidine (tempone precursor) (D??, 97%
  • 1?N, 97%)
  • 1062161-90-3
  • C28H32N8O3
  • Inhibitors
  • Akt
  • PI3K/Akt/mTOR
  • mTOR
  • PI3K