2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PROTAC
  3. EGFR PROTACs
  4. PROTAC EGFR degrader 3

PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation.

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

PROTAC EGFR degrader 3 Chemical Structure

PROTAC EGFR degrader 3 Chemical Structure

CAS No. : 2768472-28-0

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Based on 1 publication(s) in Google Scholar

PROTAC EGFR degrader 3 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation[1].

In Vitro

PROTAC EGFR degrader 3 (compound CP17) shows anti-proliferative activity of PROTACs with IC50s of 32 nM, 1.60 nM, >10000nM for H1975 (EGFRL858/T790M), HCC827 (EGFRdel19), A431 (EGFRWT) cells, respectively[1].
PROTAC EGFR degrader 3 (0, 10, 100, 1000, 10000 nM) exhibits poor cellular activity with IC50 of 481 nM, 669 nM for Ba/F3 (EGFRdel19/T790M/C797S) and Ba/F3 (EGFRL858/T790M/C797S) cells, respectively[1].
PROTAC EGFR degrader 3 (0-10000 nM) suppresses the proliferation of the PC9 (EGFRdel19/T790M/C797S) and H1975 (EGFRL858/T790M/C797S) cells, respectively[1].
PROTAC EGFR degrader 3 (30 nM; 0-72 h) decreases the expression level of EGFRL858/T790M after 8h, and degradation rate maximizes after 48 h[1].
PROTAC EGFR degrader 3 (0.3, 1, 3, 10, 100, 300 nM; 24, 48 h) induces the degradation of EGFRL858/T790M and EGFRdel19 with DC50s of 1.56 nM and 0.49 nM, respectively[1].
PROTAC EGFR degrader 3 (100, 1000 nM; 24 h) shows selective against mutant EGFR in the H1975 and HCC827 cells[1].
PROTAC EGFR degrader 3 (0.3, 1, 3, 10, 100, 300 nM; 24 h) effectively blocks EGFR singnal transduction, leading to cell proliferation inhibition[1].
PROTAC EGFR degrader 3 (30 nM) induces EGFR mutant degradation, and the lysosome is involved in the degradation process[1].

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

PROTAC EGFR degrader 3 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: H1975 (EGFRL858/T790M), HCC827 (EGFRdel19), A431 (EGFRWT) cells
Concentration:
Incubation Time: 72 h
Result: Exhibited anti-proliferative activity of PROTACs with IC50s of 32 nM, 1.60 nM, >10000nM for H1975 (EGFRL858/T790M), HCC827 (EGFRdel19), A431 (EGFRWT) cells, respectively.

Western Blot Analysis[1]

Cell Line: H1975, HCC827 cells
Concentration: 0.3, 1, 3, 10, 30 nM
Incubation Time: 24 h
Result: Remarkably decreased the phosphorylated EGFR, ERK, AKT in the H1975 and HCC827 cells.
Molecular Weight

1092.40

Formula

C60H77N13O5S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

C=CC(N1CCC[C@@H](C1)N2C3=C(N=C2NC4=CC=CC=C4)C=NC(NC5=CC=C(C=C5)N6CCN(CC6)CCCCCCCC(N[C@H](C(N7[C@@H](C[C@H](C7)O)C(N[C@H](C8=CC=C(C=C8)C9=C(N=CS9)C)C)=O)=O)C(C)(C)C)=O)=N3)=O
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 (91.54 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 0.9154 mL 4.5771 mL 9.1542 mL
5 mM 0.1831 mL 0.9154 mL 1.8308 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.

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

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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: ≥ 2.5 mg/mL (2.29 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.29 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).

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

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 (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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9154 mL 4.5771 mL 9.1542 mL 22.8854 mL
5 mM 0.1831 mL 0.9154 mL 1.8308 mL 4.5771 mL
10 mM 0.0915 mL 0.4577 mL 0.9154 mL 2.2885 mL
15 mM 0.0610 mL 0.3051 mL 0.6103 mL 1.5257 mL
20 mM 0.0458 mL 0.2289 mL 0.4577 mL 1.1443 mL
25 mM 0.0366 mL 0.1831 mL 0.3662 mL 0.9154 mL
30 mM 0.0305 mL 0.1526 mL 0.3051 mL 0.7628 mL
40 mM 0.0229 mL 0.1144 mL 0.2289 mL 0.5721 mL
50 mM 0.0183 mL 0.0915 mL 0.1831 mL 0.4577 mL
60 mM 0.0153 mL 0.0763 mL 0.1526 mL 0.3814 mL
80 mM 0.0114 mL 0.0572 mL 0.1144 mL 0.2861 mL
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PROTAC EGFR degrader 3 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:

PROTAC EGFR degrader 32768472-28-0PROTAC EGFR degrader3PROTAC EGFR degrader-3EGFRPROTACsEpidermal growth factor receptorErbB-1HER1Selectivecovalent bindinglysosomeH1975HCC827 cellsanti-proliferativenon-small-cell lung cancer (NSCLC)Inhibitorinhibitorinhibit

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