Cat. No.: HY-144605

PROTAC EGFR degrader 3

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Based on 1 Customer Validation

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.
(Pink: EGFR ligand (HY-150905); Blue: VHL ligand (HY-112078); Black: linker).

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

Purity: 97.39%
CAS No.: 2768472-28-0
Formula: C₆₀H₇₇N₁₃O₅S
Molecular Weight:1092.40

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)

PROTAC EGFR degrader 3 Chemical Structure

CAS No.: 2768472-28-0

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- Cellular Effect
- In Vitro
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

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]. (Pink: EGFR ligand (HY-150905); Blue: VHL ligand (HY-112078); Black: linker).

All PROTACs Isoforms :

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	>10000 nM Compound: CP17	Antiproliferative activity against human A-431 cells expressing EGFR wildtype assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells expressing EGFR wildtype assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35254067]
BaF3	IC₅₀	481 nM Compound: CP17	Antiproliferative activity against mouse BaF3 cells expressing EGFR deletion19/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells expressing EGFR deletion19/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay	[PMID: 35254067]
BaF3	IC₅₀	669 nM Compound: CP17	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay	[PMID: 35254067]
HCC827	IC₅₀	1.6 nM Compound: CP17	Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35254067]
HCC827	IC₅₀	1.6 nM Compound: CP17	Antiproliferative activity against human HCC827 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35254067]
NCI-H1975	IC₅₀	32 nM Compound: CP17	Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35254067]
NCI-H1975	IC₅₀	>10000 nM Compound: CP17	Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay	[PMID: 35254067]
PC-9	IC₅₀	>10000 nM Compound: CP17	Antiproliferative activity against human PC-9 cells expressing EGFR deletion19/T790M/C797S mutant assessed as reduction on cell growth growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-9 cells expressing EGFR deletion19/T790M/C797S mutant assessed as reduction on cell growth growth incubated for 72 hrs by MTT assay	[PMID: 35254067]

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 (EGFR^L858/T790M), HCC827 (EGFR^del19), A431 (EGFR^WT) 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 (EGFR^{del19/T790M/C797S}) and Ba/F3 (EGFR^{L858/T790M/C797S}) cells, respectively^[1].
PROTAC EGFR degrader 3 (0-10000 nM) suppresses the proliferation of the PC9 (EGFR^{del19/T790M/C797S}) and H1975 (EGFR^{L858/T790M/C797S}) cells, respectively^[1].
PROTAC EGFR degrader 3 (30 nM; 0-72 h) decreases the expression level of EGFR^L858/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 EGFR^L858/T790M and EGFR^del19 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.

Cell Proliferation Assay^[1]

Cell Line:

H1975 (EGFR^L858/T790M), HCC827 (EGFR^del19), A431 (EGFR^WT) cells
Concentration:
Incubation Time:

72 h
Result:

Exhibited anti-proliferative activity of PROTACs with IC₅₀s of 32 nM, 1.60 nM, >10000nM for H1975 (EGFR^L858/T790M), HCC827 (EGFR^del19), A431 (EGFR^WT) 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.

Chemical Information

CAS No. 2768472-28-0
Appearance Solid
Molecular Weight 1092.40
Formula C₆₀H₇₇N₁₃O₅S
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9154 mL

4.5771 mL

9.1542 mL

5 mM

0.1831 mL

0.9154 mL

1.8308 mL

10 mM

0.0915 mL

0.4577 mL

0.9154 mL

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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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Volume _(start) Volume _(start)

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In Vivo:

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

Stock Solution Working Solution

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.

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Zhao HY, et al. Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. J Med Chem. 2022; 65(6):4709-4726. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

PROTAC Library

All PROTACs Isoforms

All EGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PROTAC EGFR degrader 3 Related Classifications

Cat. No.: HY-144605