2. Cell Cycle/DNA Damage Apoptosis
  3. Wee1 Apoptosis
  4. WEE1-IN-7

WEE1-IN-7 (compound 12h) is a potent and orally activeWEE1 inhibitor with an IC50 value of 2.1 nM. WEE1-IN-7 induces apoptosis and cell cycle arrest at the S phase. WEE1-IN-7 shows antitumor activity.

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WEE1-IN-7

WEE1-IN-7 Chemical Structure

CAS No. : 2924006-98-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Description

WEE1-IN-7 (compound 12h) is a potent and orally activeWEE1 inhibitor with an IC50 value of 2.1 nM. WEE1-IN-7 induces apoptosis and cell cycle arrest at the S phase. WEE1-IN-7 shows antitumor activity[1].

IC50 & Target

IC50: 2.1 nM (WEE1)[1]
Cellular Effect
Cell Line Type Value Description References
A-427 IC50
84 nM
Compound: 12h
Antiproliferative activity against human A-427 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A-427 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 38847373]
LoVo IC50
82 nM
Compound: 12h
Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
[PMID: 38847373]
In Vitro

WEE1-IN-7 (compound 12h) inhibits cell viability with IC50 values of 84, 82 nM for A427, Lovo cells, respectively[1].
WEE1-IN-7 (0-800 nM; 48 h) induces apoptosis and cell cycle arrest at S phase in a dose-dependent manner[1].

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

WEE1-IN-7 Related Antibodies

Apoptosis Analysis[1]

Cell Line: A427 cells
Concentration: 200, 400, 800 nM
Incubation Time: 48 h
Result: Significantly increased the percentage of both early and late apoptotic cells in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: A427 cells
Concentration: 0, 50, 100, 200, 400 nM
Incubation Time: 48 h
Result: Induced cell cycle arrest at the S phase with the the percentage of cells in the S phase of 37.4%, 46.7%, 48.5%, 59.1%, and 59.1% at 0, 50, 100, 200, and 400 nM, respectively.
In Vivo

WEE1-IN-7 (60 mg/kg; p.o.; daily for 27 days) shows antitumor activity with the tumor growth inhibition (TGI) of 88% in Lovo CDX xenograft mice model[1].
Pharmacokinetic Parameters[1].

Admin. AUC (h·ng/mL) T1/2 (h) Vd (L/kg) CL (L/h/kg) Cmax F (%)
intravenous (1 mg/kg) 118 1.06 11.3 8.20 - -
intragastric (60 mg/kg) 4342 5.94 - - 498 61.64

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

Animal Model: Female C57 mice (Lovo CDX xenograft mice model)[1]
Dosage: 60 mg/kg
Administration: P.o.; daily for 27 days
Result: Showed antitumor activity with the tumor growth inhibition (TGI) of 88%.
Molecular Weight

520.59

Formula

C28H28N10O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=CN=C(NC3=CC=C(N4CCN(CC4)C)C=C3)N=C2N(N1CC=C)C5=CC=CC(C6=NC=CN=C6)=N5
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 : 16.67 mg/mL (32.02 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 1.9209 mL 9.6045 mL 19.2090 mL
5 mM 0.3842 mL 1.9209 mL 3.8418 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

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 1.67 mg/mL (3.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: ≥ 1.67 mg/mL (3.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
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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

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 1.9209 mL 9.6045 mL 19.2090 mL 48.0224 mL
5 mM 0.3842 mL 1.9209 mL 3.8418 mL 9.6045 mL
10 mM 0.1921 mL 0.9604 mL 1.9209 mL 4.8022 mL
15 mM 0.1281 mL 0.6403 mL 1.2806 mL 3.2015 mL
20 mM 0.0960 mL 0.4802 mL 0.9604 mL 2.4011 mL
25 mM 0.0768 mL 0.3842 mL 0.7684 mL 1.9209 mL
30 mM 0.0640 mL 0.3201 mL 0.6403 mL 1.6007 mL
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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:

WEE1-IN-72924006-98-2Wee1ApoptosisA427 cellsapoptosisS phaseLovo cellsanti-tumororally activeInhibitorinhibitorinhibit

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