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Cat. No.: HY-189915

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PROTAC EGFR degrader 20

PROTAC EGFR degrader 20 is an orally active and blood-brain barrier-penetrant EGFR PROTAC degrader. PROTAC EGFR degrader 20 binds to VHL E3 ubiquitin ligase to form a ternary complex, thereby achieving EGFR ubiquitination and PROTAC-mediated ubiquitination and proteasomal degradation of mutant EGFR. PROTAC EGFR degrader 20 selectively degrades mutant EGFR, with DC₅₀=9.14 nM against HCC827 cells (EGFR^Del19) and DC₅₀=15.2 nM against H3255 cells (EGFR^L858R). PROTAC EGFR degrader 20 inhibits tumor growth in xenograft mouse models. PROTAC EGFR degrader 20 can be used for research on non-small cell lung cancer (NSCLC).
(Pink: EGFR^del19 and EGFR^L858R ligand (HY-189916); Blue: VHL ligand (HY-189917); Black: linker).

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

Formula: C₅₅H₆₆ClF₂N₉O₇S₂
Molecular Weight:1102.75

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

PROTAC EGFR degrader 20 Chemical Structure

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC EGFR degrader 20 is an orally active and blood-brain barrier-penetrant EGFR PROTAC degrader. PROTAC EGFR degrader 20 binds to VHL E3 ubiquitin ligase to form a ternary complex, thereby achieving EGFR ubiquitination and PROTAC-mediated ubiquitination and proteasomal degradation of mutant EGFR. PROTAC EGFR degrader 20 selectively degrades mutant EGFR, with DC₅₀=9.14 nM against HCC827 cells (EGFR^Del19) and DC₅₀=15.2 nM against H3255 cells (EGFR^L858R). PROTAC EGFR degrader 20 inhibits tumor growth in xenograft mouse models. PROTAC EGFR degrader 20 can be used for research on non-small cell lung cancer (NSCLC)^[1]. (Pink: EGFR^del19 and EGFR^L858R ligand (HY-189916); Blue: VHL ligand (HY-189917); Black: linker).

IC₅₀ & Target

^[1]

EGFR^L858R

15.2 nM (DC₅₀)

EGFR^del19

9.14 nM (DC₅₀)

All PROTACs Isoforms :

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HCC827	DC₅₀	9.14 nM	EGFR degradation in human HCC827 (EGFR Del19) cells incubated 24 hrs by western blotting. EGFR degradation in human HCC827 (EGFR Del19) cells incubated 24 hrs by western blotting.	acs.jmedchem.6c01893
NCI-H3255	DC₅₀	15.2 nM	EGFR degradation in human H3255 (EGFR L858R) cells incubated 24 hrs by western blotting. EGFR degradation in human H3255 (EGFR L858R) cells incubated 24 hrs by western blotting.	acs.jmedchem.6c01893
HCC827	IC50	3.55 nM	Antiproliferative activity against human HCC827 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay. Antiproliferative activity against human HCC827 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.	acs.jmedchem.6c01893

In Vitro

Anti-cancer

PROTAC EGFR degrader 20 (compound D4) (0.03-1000 nM; 0-48 h) induces potent, selective, and sustained EGFR degradation in HCC827 (EGFR Del19) and H3255 (EGFR L858R) cells, with DC₅₀ values of 9.14 nM and 15.2 nM, respectively, while not significantly degrading wild-type EGFR in A549 cells^[1].
PROTAC EGFR degrader 20 (72 h) inhibits HCC827 cell proliferation with an IC₅₀ of 3.55 nM^[1].
PROTAC EGFR degrader 20 (500 nM; 24 h) selectively degrades EGFR in HCC827 cells without affecting other ErbB family members^[1].

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

Western Blot Analysis^[1]

Cell Line:

HCC827 (EGFR Del19), H3255 (EGFR L858R), and A549 (wild-type EGFR) cells
Concentration:

0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000, 3000, 10000 nM (HCC827 and H3255, 24 h)
30, 100, 300 nM (HCC827, 24 h)
30 nM (HCC827, up to 48 h)
Incubation Time:

24 h (HCC827, H3255, and A549)
0, 3, 6, 12, 24, 48 h (HCC827 kinetic)
Result:

Achieved EGFR degradation in HCC827 cells with DC₅₀ = 9.14 nM and D_max = 98%.
Reached 70%, 90%, and 97% EGFR degradation in HCC827 cells at 30, 100, and 300 nM, respectively, after 24 h.
Produced EGFR degradation in H3255 cells with DC₅₀ = 15.2 nM and D_max = 98%.
Detected no significant degradation of wild‑type EGFR in A549 cells.
Observed >80% reduction of EGFR levels within 6 h and >90% degradation sustained for up to 48 h at 30 nM in kinetic analysis.

Parmacokinetics

Species	Dose	Route	T_max	C_max	T_1/2	AUC_last	AUC_inf	F	CL	V_ss
Mice^[1]	5 mg/kg	i.v.	/	5.56 × 10⁴ ng/mL	8.48 h	3.23 × 10⁴ ng·h/mL	3.40 × 10⁴ ng·h/mL	/	2.45 mL/min/kg	659 mL/kg
Mice^[1]	30 mg/kg	p.o.	2.00 h	3.15 × 10³ ng/mL	6.49 h	2.18 × 10⁴ ng·h/mL	2.37 × 10⁴ ng·h/mL	11.3 %	/	/

In Vivo

Anti-cancer

PROTAC EGFR degrader 20 (compound D4) (15 mg/kg; PO; QD; 14 days) inhibits tumor growth in the HCC827 xenograft mouse model^[1].

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

Animal Model:

BALB/c nude (female, 6-8 weeks old, inoculated into the left axilla with a mixture of HCC827 cells (5×10⁶ cells) and Matrigel in 100 μL of PBS)^[1]
Dosage:

15 mg/kg
Administration:

PO; QD; for 14 days
Result:

Resulted in complete tumor growth inhibition (TGI = 101%).

Related Protocols :

Chemical Information

Molecular Weight 1102.75
Formula C₅₅H₆₆ClF₂N₉O₇S₂
SMILES

FC1=C(C=CC=C1NC2=NC=NC3=C2C=C(C(OC)=C3)OC(N4[C@@H](CN(CC4)C[C@H]5CC[C@@H](CC5)CSC(C)([C@@H](C(N6[C@@H](C[C@H](C6)O)C(N[C@H](C7=CC=C(C=C7)C8=C(N=CS8)C)C)=O)=O)NC(C9(CC9)F)=O)C)C)=O)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Ni X, et al. Discovery of Potent and Selective VHL‑Recruiting PROTAC Degraders Targeting EGFR with Improved Developability and Potent Anti‑NSCLC Efficacy. Journal of Medicinal Chemistry. 2026;69(19):22671‑22698.

Calculators

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

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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.

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