Reagents and instruments for immunology, cell biology and molecular biology.
 
> PROTAC EGFR degrader 2 [3031336-58-7]

PROTAC EGFR degrader 2 [3031336-58-7]

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Cat# HY-144304-25mg

Size : 25mg

Brand : MedChemExpress

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Description

PROTAC EGFR degrader 2 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 2 exhibits excellent antiproliferative activity with IC50 of 4.0 nM and good EGFR degradation activity with DC50 of 36.51 nM. PROTAC EGFR degrader 2 can be used for the synthesis of nitroreductase (NTR)-responsive PROTAC[1].

IC50 & Target[1]

EGFR

36.51 nM (DC50)

Cellular Effect
Cell Line Type Value Description References
HCC827 IC50
18.7 nM
Compound: 17
Antiproliferative activity against human HCC827 cells assessed as cell viability measured after 72 hrs under hypoxic condition by CCK-8 assay
Antiproliferative activity against human HCC827 cells assessed as cell viability measured after 72 hrs under hypoxic condition by CCK-8 assay
[PMID: 35175763]
HCC827 IC50
4 nM
Compound: 17
Antiproliferative activity against human HCC827 cells assessed as reduction in cell viability measured after 72 hrs under normoxic condition by CCK-8 assay
Antiproliferative activity against human HCC827 cells assessed as reduction in cell viability measured after 72 hrs under normoxic condition by CCK-8 assay
[PMID: 35175763]
HCC827 IC50
6 nM
Compound: 17
Antiproliferative activity against human HCC827 cells assessed as cell viability measured after 72 hrs in presence of NTR by CCK-8 assay
Antiproliferative activity against human HCC827 cells assessed as cell viability measured after 72 hrs in presence of NTR by CCK-8 assay
[PMID: 35175763]
Molecular Weight

1151.78

Formula

C58H72ClFN12O8S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

FC(C=CC(NC1=NC=NC2=CC(OCCCCCC3=CN(N=N3)CCOCCOCC(N[C@H](C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)O)=O)C(C)(C)C)=O)=C(C=C21)NC(/C=C/CN7CCCCC7)=O)=C8)=C8Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (86.82 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 0.8682 mL 4.3411 mL 8.6822 mL
5 mM 0.1736 mL 0.8682 mL 1.7364 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 (2.17 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.
Purity & Documentation
References