PROTAC EGFR degrader 14

Name: PROTAC EGFR degrader 14
Brand: MedChemExpress
SKU: HY-175252
Rating: 4.5 (1 reviews)

Cat. No.: HY-175252 Purity: 99.26%: Data Sheet
COA

SDS
Handling Instructions
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PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC₅₀ of about 2.9 nM and a D_max of 93.1% for EGFR^{L858R/T790M/C797S}. PROTAC EGFR degrader 14 selectively induces EGFR^C797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFR^WT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688)).

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

PROTAC EGFR degrader 14 Chemical Structure

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PROTACs Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All EGFR Isoform Specific Products:

View All Isoforms

EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

VHL

In Vitro

PROTAC EGFR degrader 14 (Compound 9ea) (0-20 μM, 0-24 h) concentration- and dose-dependently degrades EGFR in PC9 (EGFR^{L858R/T790M/C797S}) and PC9 (EGFR^{Del19/T790M/C797S}) cells, with DC₅₀ values of 2.9 and 21.6 nM respectively and is inactive in the EGFR wild-type cell line (A549, DC₅₀ = 2157 nM)^[1].
PROTAC EGFR degrader 14 (0.1-5 μM, 24-48 h) induces G1 phase arrest and cell apoptosis in PC9 (EGFR^{L858R/T790M/C797S}) and PC9 (EGFR^{Del19/T790M/C797S}) cells ^[1].
PROTAC EGFR degrader 14 (0.01-0.25 μM, 24 h) effectively reduces EGFR degradation and it depends on the proteasome and VHL system in PC9 (EGFR^{L858R/T790M/C797S}) and PC9 (EGFR^{Del19/T790M/C797S}) cells ^[1].

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

Cell Cycle Analysis^[1]

Cell Line:	PC9 (EGFR^{L858R/T790M/C797S}) and PC9 (EGFR^{Del19/T790M/C797S}) cells
Concentration:	0.1, 0.5, 1 and 5 μM
Incubation Time:	24 h
Result:	Increased the percentages of cells in the G1/G0 phase concentration-dependently. Reduced the S phase populations 24.8% to 10.4% in PC9 (EGFR^{L858R/T790M/C797S}) cells and 22.3% to 10.9% in PC9 (EGFR^{Del19/T790M/C797S}) cells.

Apoptosis Analysis^[1]

Cell Line:	PC9 (EGFR^{L858R/T790M/C797S}) and PC9 (EGFR^{Del19/T790M/C797S}) cells
Concentration:	0.1, 0.5, 1 and 5 μM
Incubation Time:	48 h
Result:	Significantly promoted cell apoptosis in a concentration-dependent manner. Reached the apoptotic rates of 22.0% and 36.5%, respectively.

Western Blot Analysis^[1]

Cell Line:	PC9 (EGFR^{L858R/T790M/C797S}) and PC9 (EGFR^{Del19/T790M/C797S}) cells
Concentration:	0.01, 0.05, 0.25 μM
Incubation Time:	24 h
Result:	Effectively inhibited downstream signaling proteins as the phosphorylation of STAT3, AKT and ERK1/2. Showed weaker inhibition of EGFR and downstream signaling proteins in A549 cells.

Western Blot Analysis^[1]

Cell Line:	PC9 (EGFR^{L858R/T790M/C797S}), PC9 (EGFR^{Del19/T790M/C797S}) cells and A549 (EGFR^WT)
Concentration:	0.25 μM pretreated with MG132 (HY-13259) (10 μM), MLN4924 (HY-70062) (10 μM), and VHL ligand (10 μM and 20 μM) for 4 h
Incubation Time:	24 h
Result:	Effectively blocked EGFR degradation by pretreatment with the proteasome inhibitor MG132 or the E1 neddylation inhibitor MLN4924. Exhibited no effect in inducing EGFR degradation without VHL ligand.

In Vivo

PROTAC EGFR degrader 14 (Compound 9ea) (25-50 mg/kg, i.v., every other day, for 15 days) significantly inhibits tumor growth in PC9 (EGFR^{L858R/T790M/C797S}) xenografts mice model, with potent EGFR degradation efficacy and no signs of toxicity^[1].

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

Animal Model:	PC9 (EGFR^{L858R/T790M/C797S}) xenografts model in male BALB/c nude mice^[1]
Dosage:	25 and 50 mg/kg
Administration:	Intravenous injection (i.v.), every other day, for 15 days
Result:	Demonstrated superior efficacy with the tumor growth inhibition (TGI) rate of 74.7%. No statistically significant body weight loss was observed in mice during the treatment period. Significantly reduced the average tumor weight. Displayed no toxicity on the primary organs, including the heart, liver, spleen, lungs, kidneys, and brain. Caused no significant changes in blood parameters analysis and blood biochemistry profiling.

Molecular Weight

1008.33

Formula

C₅₇H₇₃N₁₁O₄S

Appearance

Solid

Color

White to light yellow

SMILES

O=C(CCCCCCN1CCN(C2=CC=C(NC3=NC=C4C(N(C(CNC5=CC=CC=C5)=C4)C6CCCC6)=N3)C=C2)CC1)N[C@@H](C(C)(C)C)C(N7[C@H](C(NCC8=CC=C(C9=C(C)N=CS9)C=C8)=O)C[C@@H](O)C7)=O

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 : 100 mg/mL (99.17 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	0.9917 mL	4.9587 mL	9.9174 mL
5 mM	0.1983 mL	0.9917 mL	1.9835 mL
10 mM	0.0992 mL	0.4959 mL	0.9917 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.26%

Select Batch:

Data Sheet (278 KB) SDS (251 KB)

COA (247 KB) HNMR (164 KB) RP-HPLC (173 KB) LCMS (239 KB)

Handling Instructions (2659 KB)

References

[1]. Wang X, et al. Discovery of a Novel EGFR PROTAC Degrader against C797S Resistance Mutation with Potent Antitumor Efficacy in NSCLC Treatment. J Med Chem. 2025 Jul 24;68(14):14569-14593. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	0.9917 mL	4.9587 mL	9.9174 mL	24.7935 mL
	5 mM	0.1983 mL	0.9917 mL	1.9835 mL	4.9587 mL
	10 mM	0.0992 mL	0.4959 mL	0.9917 mL	2.4793 mL
	15 mM	0.0661 mL	0.3306 mL	0.6612 mL	1.6529 mL
	20 mM	0.0496 mL	0.2479 mL	0.4959 mL	1.2397 mL
	25 mM	0.0397 mL	0.1983 mL	0.3967 mL	0.9917 mL
	30 mM	0.0331 mL	0.1653 mL	0.3306 mL	0.8264 mL
	40 mM	0.0248 mL	0.1240 mL	0.2479 mL	0.6198 mL
	50 mM	0.0198 mL	0.0992 mL	0.1983 mL	0.4959 mL
	60 mM	0.0165 mL	0.0826 mL	0.1653 mL	0.4132 mL
	80 mM	0.0124 mL	0.0620 mL	0.1240 mL	0.3099 mL