PROTAC EGFR degrader 3

Name: PROTAC EGFR degrader 3
Brand: MedChemExpress
SKU: HY-144605
Rating: 4.5 (1 reviews)

Cat. No.: HY-144605 Purity: 97.39%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 2768472-28-0

Size	Price	Stock	Quantity
1 mg	USD 860	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 2150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 3450	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

Molecular Weight

1092.40

Formula

C₆₀H₇₇N₁₃O₅S

CAS No.

2768472-28-0

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
10 mM	0.0915 mL	0.4577 mL	0.9154 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

Purity: 97.39%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (250 KB) HNMR (216 KB) RP-HPLC (244 KB) LCMS (93 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]

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