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Cat. No.: HY-174415

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ZSH-2117

ZSH-2117 is an NEDD4-recruiting EGFR PROTAC degrader. ZSH-2117 shows an IC₅₀ of 13 nM against EGFR^{L858R/T790M/C797S}, induces EGFR proteasome-dependent degradation, inhibits the downstream signaling pathways of EGFR, including the phosphorylation of AKT and ERK, suppresses cancer cell proliferation, and exhibits in vivo anti-tumor activity. ZSH-2117 can be used in research related to non-small cell lung cancer.
(Pink: EGFR ligand (HY-175162); Blue: NEDD4 ligand (HY-175159); Black: linker).

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Formule: C₃₆H₃₉BrClN₈O₂P
Masse moléculaire:762.08

Stockage:

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

Data Sheet (284 KB)

ZSH-2117 Chemical Structure

Stock

Quantité

Amount: USD 0.00

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Use of MCE Products

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

ZSH-2117 is an NEDD4-recruiting EGFR PROTAC degrader. ZSH-2117 shows an IC₅₀ of 13 nM against EGFR^{L858R/T790M/C797S}, induces EGFR proteasome-dependent degradation, inhibits the downstream signaling pathways of EGFR, including the phosphorylation of AKT and ERK, suppresses cancer cell proliferation, and exhibits in vivo anti-tumor activity. ZSH-2117 can be used in research related to non-small cell lung cancer^[1]. (Pink: EGFR ligand (HY-175162); Blue: NEDD4 ligand (HY-175159); Black: linker).

IC₅₀ & Target

^[1]

EGFR^{L858R/T790M/C797S}

13 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform PROTACs :

Voir tous les produits spécifiques à Isoform EGFR :

Voir tous les produits spécifiques à Isoform Akt :

Voir tous les produits spécifiques à Isoform ERK :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	DC₅₀	45 nM	Half-maximal degradation concentration of EGFR^{L858R/T790M/C797S} in Ba/F3-EGFR^{L858R/T790M/C797S} cells assessed by Western blot analysis after 8 h of treatment. Half-maximal degradation concentration of EGFR^{L858R/T790M/C797S} in Ba/F3-EGFR^{L858R/T790M/C797S} cells assessed by Western blot analysis after 8 h of treatment.	40506832
NCI-H1975	DC₅₀	149 nM	Half-maximal degradation concentration of FLAG-EGFR^{L858R/T790M/C797S} in H1975-FLAG-EGFR^{L858R/T790M/C797S} cells assessed by Western blot analysis after 8 h of treatment. Half-maximal degradation concentration of FLAG-EGFR^{L858R/T790M/C797S} in H1975-FLAG-EGFR^{L858R/T790M/C797S} cells assessed by Western blot analysis after 8 h of treatment.	40506832
BaF3	IC50	13 nM	Half-maximal inhibitory concentration for proliferation inhibition in Ba/F3-EGFR^{L858R/T790M/C797S} cells assessed via cell viability measurement. Half-maximal inhibitory concentration for proliferation inhibition in Ba/F3-EGFR^{L858R/T790M/C797S} cells assessed via cell viability measurement.	40506832

In Vitro

ZSH-2117 (0.001-100 μM) potently inhibits the proliferation of Ba/F3-EGFR^{L858R/T790M/C797S} cells, with an IC₅₀ of 13 nM^[1].
ZSH-2117 (0.2 μM; 8 h) potently degrades EGFR^{L858R/T790M/C797S} in Ba/F3-EGFR^{L858R/T790M/C797S} cells^[1].
ZSH-2117 (25-200 nM; 8 h) potently induces concentration-dependent degradation of EGFR^{L858R/T790M/C797S} in Ba/F3-EGFR^{L858R/T790M/C797S} cells, with a DC₅₀ of 45 nM and a maximum degradation rate of 96%^[1].
ZSH-2117 (100 nM; 10 h)-mediated degradation of EGFR^{L858R/T790M/C797S} in Ba/F3-EGFR^{L858R/T790M/C797S} cells relies on the proteasome, the activity of E1 ligase, and requires binding to EGFR^{L858R/T790M/C797S}^[1].
ZSH-2117 (0.5 μM; 3 h) competes with probe AZ9-1 for binding to the E3 ligase NEDD4 in Ba/F3-EGFR^{L858R/T790M/C797S} cells^[1].
ZSH-2117 (0.1-3 μM; 8 h) potently induces concentration-dependent degradation of FLAG-EGFR^{L858R/T790M/C797S} in H1975-FLAG-EGFR^{L858R/T790M/C797S} cells, with a DC₅₀ of 149 nM and a maximum degradation rate of 94%^[1].
The NEDD4-dependent degradation of FLAG-EGFR^{L858R/T790M/C797S} mediated by ZSH-2117 (0.2 μM; 8 h) occurs in H1975-FLAG-EGFR^{L858R/T790M/C797S} cells^[1].
ZSH-2117 (0.2 μM; 8 h)-mediated degradation of FLAG-EGFR^{L858R/T790M/C797S} and formation of the EGFR-NEDD4 ternary complex in H1975-FLAG-EGFR^{L858R/T790M/C797S} cells depend on the C1286 residue of NEDD4^[1].
ZSH-2117 (0.5 μM; 4 h) covalently binds to the cysteine residue C1286 on the surface of NEDD4 in H1975 cells expressing HA-NEDD4-EGFR^{L858R/T790M/C797S}^[1].
ZSH-2117 (25-500 nM; 8 h) inhibits the downstream signaling pathways of EGFR (phosphorylation of AKT and ERK) in Ba/F3-EGFR^{L858R/T790M/C797S} cells in a concentration-dependent manner in vitro, and simultaneously induces the degradation of EGFR^{L858R/T790M/C797S}^[1].

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

Western Blot Analysis^[1]

Cell Line:

Ba/F3-EGFR^{L858R/T790M/C797S}
Concentration:

0.2 μM
Incubation Time:

8 h
Result:

Exhibited the highest degradation activity for EGFR^{L858R/T790M/C797S} among tested analogs.
Reduced protein levels to a significantly lower percentage of control than DMSO, ZSH-1136, ZSH-2155, ZSH-2158, and ZSH-3005.

Western Blot Analysis^[1]

Cell Line:

Ba/F3-EGFR^{L858R/T790M/C797S}
Concentration:

25, 50, 100, 200 nM
Incubation Time:

8 h
Result:

Induced concentration-dependent degradation of EGFR^{L858R/T790M/C797S}.
Achieved a half-maximal degradation concentration (DC₅₀) of 45 nM.
Reached a maximum degradation (D_max) of 96%.

Western Blot Analysis^[1]

Cell Line:

Ba/F3-EGFR^{L858R/T790M/C797S}
Concentration:

100 nM
Incubation Time:

10 h
Result:

Attenuated EGFR^{L858R/T790M/C797S} degradation.
Showed no effect on EGFR^{L858R/T790M/C797S} degradation.
Blocked EGFR^{L858R/T790M/C797S} degradation.

Western Blot Analysis^[1]

Cell Line:

H1975-FLAG-EGFR^{L858R/T790M/C797S}
Concentration:

0.1, 0.3, 1, 3 μM
Incubation Time:

8 h
Result:

Induced concentration-dependent degradation of FLAG-EGFR^{L858R/T790M/C797S}.
Achieved a half-maximal degradation concentration (DC₅₀) of 149 nM.
Reached a maximum degradation (D_max) of 94%.

Western Blot Analysis^[1]

Cell Line:

H1975-FLAG-EGFR^{L858R/T790M/C797S}
Concentration:

0.2 μM
Incubation Time:

8 h
Result:

Completely eliminated ZSH-2117-induced degradation of FLAG-EGFR^{L858R/T790M/C797S} with knockdown of NEDD4.
Showed significant degradation of FLAG-EGFR^{L858R/T790M/C797S} in shScramble control cells.
Completely blocked ZSH-2117-induced degradation of FLAG-EGFR^{L858R/T790M/C797S} with NEDD4 C1286A mutant.
Abolished the interaction between NEDD4 and FLAG-EGFR^{L858R/T790M/C797S} with NEDD4 C1286A mutant.

Western Blot Analysis^[1]

Cell Line:

Ba/F3-EGFR^{L858R/T790M/C797S}
Concentration:

25, 50, 100, 200, 500 nM
Incubation Time:

8 h
Result:

Induced concentration-dependent reductions in p-EGFR, p-AKT(S473), and p-ERK levels.
Corresponded reduced EGFR^{L858R/T790M/C797S} protein levels with decreased downstream signaling levels.

In Vivo

ZSH-2117 (2.5 mg/kg; i.p.; administered on days 0, 3, 5 and 7) exhibits potent in vivo antitumor activity in Ba/F3-EGFR^{L858R/T790M/C797S} xenograft mice, with a 65% tumor growth inhibition rate, while maintaining minimal effects on body weight^[1].

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

Animal Model:

NOD-SCID mice^[1]
Dosage:

2.5 mg/kg
Administration:

i.p.; administered on days 0, 3, 5 and 7
Result:

Achieved a tumor growth inhibition (TGI) rate of 65%.
Significantly reduced tumor volume and tumor weight relative to vehicle control.
Degraded EGFRL858R/T790M/C797S protein in tumor tissues.
Had minimal impact on mouse body weight.

Chemical Information

Masse moléculaire 762.08
Formule C₃₆H₃₉BrClN₈O₂P
SMILES

O=C(N1CCN(C2CCN(C3=CC=C(NC4=NC=C(Cl)C(NC5=CC=CC=C5P(C)(C)=O)=N4)C=C3Br)CC2)CC1)C6N=C6C7=CC=CC=C7
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (284 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)
Instruction de manipulation (2659 KB)

Références

[1]. He X, et al. Covalent Recruitment of NEDD4 for Targeted Protein Degradation: Rational Design of Small Molecular Degraders. Journal of the American Chemical Society. 2025 Jun 25;147(25):21512-21525. [Content Brief]

Calculators

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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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MOQ

Minimum order quantity

100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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ZSH-2117

Voir tous les produits spécifiques à Isoform PROTACs

Voir tous les produits spécifiques à Isoform EGFR

Voir tous les produits spécifiques à Isoform Akt

Voir tous les produits spécifiques à Isoform ERK

Activité biologique

Description

IC50 & Target

Cellular Effect

In Vitro

In Vivo

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

ZSH-2117 Related Classifications

HY-174415 Related Classifications

Bioz

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