2. PI3K/Akt/mTOR
  3. mTOR PI3K
  4. WYE-687

WYE-687 is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.

For research use only. We do not sell to patients.

WYE-687 Chemical Structure

WYE-687 Chemical Structure

CAS No. : 1062161-90-3

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5 mg USD 70 In-stock
10 mg USD 112 In-stock
25 mg USD 235 In-stock
50 mg USD 376 In-stock
100 mg USD 602 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of WYE-687:

WYE-687 Related Antibodies

Top Publications Citing Use of Products

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mTOR mTORC1 mTORC2

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

WYE-687 is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.

IC50 & Target[1][2]

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)

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
4.6 nM
Compound: 9
Inhibition of flag-tagged truncated human mTOR (1360-2549) expressed in HEK293 cells by DELFIA assay
Inhibition of flag-tagged truncated human mTOR (1360-2549) expressed in HEK293 cells by DELFIA assay
[PMID: 19645448]
LNCaP IC50
213 nM
Compound: 22a
Antiproliferative activity against human LNCAP cells after 3 days by MTS assay
Antiproliferative activity against human LNCAP cells after 3 days by MTS assay
[PMID: 19894727]
LNCaP IC50
213 nM
Compound: 9
Cytotoxicity against human LNCAP cells after 3 days by MTS assay
Cytotoxicity against human LNCAP cells after 3 days by MTS assay
[PMID: 19645448]
In Vitro

In the DELFIA measuring His6-S6K1 T389 phosphorylation, WYE-687 inhibits recombinant mTOR enzyme with an IC50 of 7 nM[1]. HL-60 AML cells are treated with applied concentrations of WYE-687 (33-1000 nM), MTT cell survival assay results demonstrate that WYE-687 potently inhibits HL-60 cell survival in a dose-dependent manner. A time dependent response by WYE-687 is also noticed. The number of dead (“trypan blue” positive) HL-60 cells is significantly increased following applied WYE-687 (100-1000 nM) treatment. At the meantime, HL-60 cell proliferation, tested by [H3] Thymidine integration assay, is also inhibited by the WYE-687. Results show that WYE-687 is also antisurvival (“cytotoxic”) to the other AML cell lines: U937, THP-1 and AML-193[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

WYE-687 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

528.61

Formula

C28H32N8O3
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(OC)NC1=CC=C(C2=NC(N3CCOCC3)=C4C(N(C5CCN(CC6=CC=CN=C6)CC5)N=C4)=N2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (47.29 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8918 mL 9.4588 mL 18.9175 mL
5 mM 0.3784 mL 1.8918 mL 3.7835 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Kinase Assay
[1]

The routine inhibitor assays are performed in 96-well plates for 2 h at room temperature in 25 μL containing 6 nM Flag-TOR(3.5) (estimated 5-10% purity), 1 μM His6-S6K and 100 μM ATP. The assays are performed and detected by DELFIA employing the Euphospho-p70S6K T389 antibody. Some assays employ a commercially purchased batch of mTOR. For inhibitor versus ATP matrix competition, mTOR kinase reactions are carried out with varying concentrations of ATP (0, 25, 50 100, 200, 400 and 800 μM) in combination with varying concentrations of inhibitor. The assays contain 12 nM Flag-TOR(3.5), 1 μM His-S6K and are incubated for 30 min. The assay results are similarly detected by DELFIA and processed for generation of double-reciprocal plots[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

Acute myeloid leukemia (AML) cells/progenitor cells are seeded at a density of 1 ×105 cells/well in 0.5 mL DMEM containing 10% FBS onto the 48-well tissue culture plates, cells are treated with indicated concentrations of WYE-687 (33-1000 nM) with the presence of 1 mCi/mL of tritiated thymidine. To determine [H3] thymidine incorporation, cells are washed, the DNA is precipitated with cold 10% trichloroacetic acid (TCA), solubilized with 1.0 M sodium hydroxide, and aliquots are counted by liquid-scintillation spectrometry. The value of treatment group is normalized to that of untreated control group[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
U937 cells (2×106 cells/mice, suspended in 100 mL of culture medium) are injected into the right flanks of 6-week-old male CB17 severe combined immunodeficient (SCID)/beige mice, and cells are allowed to grow to palpable tumors. When tumors reach a volume around 100 mm3, animals are randomly assigned to three groups: WYE-687 (5 mg/kg body weight), WYE- 687 (25 mg/kg body weight) or the vehicle control (5% ethanol, 2% Tween 80, and 5% polyethylene glycol-400). WYE-687 and vehicle control are freshly prepared, and given by oral gavage daily for 7 consecutive days. Tumor sizes are measured. At the end of experiment, the animals are killed, and the tumors are removed and weighted.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8918 mL 9.4588 mL 18.9175 mL 47.2938 mL
5 mM 0.3784 mL 1.8918 mL 3.7835 mL 9.4588 mL
10 mM 0.1892 mL 0.9459 mL 1.8918 mL 4.7294 mL
15 mM 0.1261 mL 0.6306 mL 1.2612 mL 3.1529 mL
20 mM 0.0946 mL 0.4729 mL 0.9459 mL 2.3647 mL
25 mM 0.0757 mL 0.3784 mL 0.7567 mL 1.8918 mL
30 mM 0.0631 mL 0.3153 mL 0.6306 mL 1.5765 mL
40 mM 0.0473 mL 0.2365 mL 0.4729 mL 1.1823 mL
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WYE-687 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WYE-6871062161-90-3WYE687WYE 687mTORPI3KMammalian target of RapamycinPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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