1. Cell Cycle/DNA Damage PROTAC
  2. Wee1 PROTACs
  3. Pomalidomide-C3-adavosertib

Pomalidomide-C3-adavosertib is a rapid and selective PROTAC Wee1 degrader (IC50=3.58 nM). Pomalidomide-C3-adavosertib shows anti-cancer cell proliferation activity, and induces apoptosis.

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

Pomalidomide-C3-adavosertib Chemical Structure

Pomalidomide-C3-adavosertib Chemical Structure

CAS No. : 2414418-49-6

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Based on 1 publication(s) in Google Scholar

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Description

Pomalidomide-C3-adavosertib is a rapid and selective PROTAC Wee1 degrader (IC50=3.58 nM). Pomalidomide-C3-adavosertib shows anti-cancer cell proliferation activity, and induces apoptosis[1].

In Vitro

Pomalidomide-C3-adavosertib (1 nM-10 μM; 24, 48, and 72 h) induces CRBN-dependent anti-proliferative effects and synergized with Olaparib[1].
Pomalidomide-C3-adavosertib (100 nM; 24 h) induces DNA damage, apoptosis, and deregulation of the G2/M checkpoint[1].
Pomalidomide-C3-adavosertib (1 nM-10 μM; 6 h) degrades Wee1 in MOLT4 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: OVCAR8, COV362, and Kuramochi cells
Concentration: 1 nM-10 μM
Incubation Time: 24, 48, and 72 hours
Result: Degraded Wee1 in OVCAR8 cells, with maximal degradation observed at a 100 nM treatment.

Cell Cycle Analysis[1]

Cell Line: MOLT4 cells
Concentration: 100 nM
Incubation Time: 24 hours
Result: Led to reduced pCDKl Y15, increased apoptosis, and increased unrepaired DNA.

Western Blot Analysis[1]

Cell Line: MOLT4 cells
Concentration: 1 nM-10 μM
Incubation Time: 6 hours
Result: Degraded Wee1 after a 6-hour treatment in MOLT4 cells, and induced the downstream changes expected from Wee1 loss-including a decrease in phosphorylated cyclin-dependent kinase 1 (pCDK1) and an increase in pH 3.
Molecular Weight

799.88

Formula

C42H45N11O6

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N(CC=C)N(C2=NC(C(O)(C)C)=CC=C2)C3=NC(NC4=CC=C(N5CCN(CCCNC6=CC=CC(C(N7C8CCC(NC8=O)=O)=O)=C6C7=O)CC5)C=C4)=NC=C31

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 : 50 mg/mL (62.51 mM; Need ultrasonic; 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 1.2502 mL 6.2509 mL 12.5019 mL
5 mM 0.2500 mL 1.2502 mL 2.5004 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.

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  • Dilution Calculator

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: ≥ 1.25 mg/mL (1.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
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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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 1.2502 mL 6.2509 mL 12.5019 mL 31.2547 mL
5 mM 0.2500 mL 1.2502 mL 2.5004 mL 6.2509 mL
10 mM 0.1250 mL 0.6251 mL 1.2502 mL 3.1255 mL
15 mM 0.0833 mL 0.4167 mL 0.8335 mL 2.0836 mL
20 mM 0.0625 mL 0.3125 mL 0.6251 mL 1.5627 mL
25 mM 0.0500 mL 0.2500 mL 0.5001 mL 1.2502 mL
30 mM 0.0417 mL 0.2084 mL 0.4167 mL 1.0418 mL
40 mM 0.0313 mL 0.1563 mL 0.3125 mL 0.7814 mL
50 mM 0.0250 mL 0.1250 mL 0.2500 mL 0.6251 mL
60 mM 0.0208 mL 0.1042 mL 0.2084 mL 0.5209 mL
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    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.

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Product Name:
Pomalidomide-C3-adavosertib
Cat. No.:
HY-133618
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