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Cat. No.: HY-175321

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PROTAC c-Met degrader-6

PROTAC c-Met degrader-6 is a potent and orally active c-Met PROTACdegrader. PROTAC c-Met degrader-6 significantly induces the degradation of the c-Met protein with DC₅₀s of 0.52 nM and 0.45 nM in EBC-1 and Hs746T. PROTAC c-Met degrader-6 almost abrogates the migratory and invasion abilities of tumor cells and significantly induces the apoptosis and blocks the cell cycle in the G0/G1 phase. PROTAC c-Met degrader-6 can be used for the study of various cancers such as non-small cell lung cancer and stomach cancer.
(Pink: c-Met ligand (HY-W425461); Blue: Cereblon ligand (HY-14658); Black: linker (HY-20797)).

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

Formula: C₄₁H₃₅N₉O₆
Molecular Weight:749.77

Storage:

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

Data Sheet (272 KB)

PROTAC c-Met degrader-6 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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

Biological Activity

Description

PROTAC c-Met degrader-6 is a potent and orally active c-Met PROTACdegrader. PROTAC c-Met degrader-6 significantly induces the degradation of the c-Met protein with DC₅₀s of 0.52 nM and 0.45 nM in EBC-1 and Hs746T. PROTAC c-Met degrader-6 almost abrogates the migratory and invasion abilities of tumor cells and significantly induces the apoptosis and blocks the cell cycle in the G0/G1 phase. PROTAC c-Met degrader-6 can be used for the study of various cancers such as non-small cell lung cancer and stomach cancer^[1]. (Pink: c-Met ligand (HY-W425461); Blue: Cereblon ligand (HY-14658); Black: linker (HY-20797)).

IC₅₀ & Target^[1]

c-Met

All PROTACs Isoforms :

In Vitro

PROTAC c-Met degrader-6 (Compound G4) (72 h) exhibits antiproliferation efficacy with IC₅₀ values of 3.55, 3.01, and 7.48 nM on EBC-1, Hs746T, and MHCC97H cells, respectively^[1].
PROTAC c-Met degrader-6 (5-10 nM, 24-48 h) exhibits strong effects on inducing cell apoptosis, G1 cell cycle arrest, and inhibiting cell migration and invasion^[1].
PROTAC c-Met degrader-6 (1-10 nM, 48 h) significantly degrades c-Met through the ubiquitin proteasome pathway in EBC-1 and Hs746T cells^[1].
PROTAC c-Met degrader-6 (100-1000 nM, 48 h-3 days) exhibits excellent antiproliferative against EBC-1 and Hs746T cells with c-MetD1228N and c-MetY1230H mutants^[1].
PROTAC c-Met degrader-6 exhibits good metabolic stability in the human liver microsome and mouse liver microsome^[1].

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

Apoptosis Analysis^[1]

Cell Line:

EBC-1 and Hs746T cells
Concentration:

10 nM
Incubation Time:

48 h
Result:

Produced the apoptosis rates of 21.8% in EBC-1 and observed similar results in Hs746T.

Cell Cycle Analysis^[1]

Cell Line:

EBC-1 and Hs746T cells
Concentration:

10 nM
Incubation Time:

48 h
Result:

Induced cell cycle arrest at the G0/G1 phase.

Cell Migration Assay ^[1]

Cell Line:

EBC-1 and Hs746T cells
Concentration:

5 nM
Incubation Time:

24 h
Result:

Significantly inhibited the migratory capacity.

Cell Invasion Assay^[1]

Cell Line:

EBC-1 and Hs746T cells
Concentration:

5 nM
Incubation Time:

24 h
Result:

Significantly inhibited the invasive capacity.

Western Blot Analysis^[1]

Cell Line:

EBC-1 and Hs746T cells
Concentration:

1 and 10 nM
Incubation Time:

48 h
Result:

Significantly inhibited the levels of c-Met phosphorylation (p-c-Met) and STAT3 phosphorylation (p-STAT3) at 1nM
Completely blocked the c-Met degradation effect pretreatment with MLN4924 (E1 ubiquitin-activating enzyme inhibitor) (HY-70062) and MG132 (proteasome inhibitor) (HY-13259).

Western Blot Analysis^[1]

Cell Line:

EBC-1 and Hs746T cells harboring a D1228N mutation
Concentration:

100 and 1000 nM
Incubation Time:

48 h
Result:

Inhibited the p-c-Met level, and complete c-Met degradation and p-c-Met inhibition.

Parmacokinetics

Species	Dose	Route	T_1/2	AUC_0-t	AUC_0-∞	V_ss	CL	T_max	C_max	F
Rat^[1]	1 mg/kg	i.v.	4.94 h	1262.8 ng·h/mL	1298.9 ng·h/mL	3.9 L/kg	0.79 L/h/kg	/	/	/
Rat^[1]	20 mg/kg	p.o.	11.42 h	1848.0 ng·h/mL	1929.9 ng·h/mL	/	/	1.80 h	156.0 ng/mL	7.43 %

In Vivo

PROTAC c-Met degrader-6 (Compound G4) (5-10 mg/kg, p.o., once daily for 18 days) significantly inhibits tumor growth in EBC-1 xenografts mice model^[1].

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

Animal Model:

EBC-1 xenografts model established in NOD/SCID mice (6 week-old)^[1]
Dosage:

5 and 10 mg/kg
Administration:

Orally administration (p.o.), once daily for 18 days
Result:

Significantly inhibited EBC-1 tumor growth, with tumor growth inhibition (TGI %) values of 84.12% at 5 mg/kg and 99.28% at 10 mg/kg after 10 days
Demonstrated complete tumor inhibition during the extended period (by day 18) at 10 mg/kg.
Exhibited a notable reduction in the percentage of Ki67-and CD31-positive tumor cells and an Increased percentage of cleaved caspase 3-positive tumor cells.
Exhibited more potent effects on reducing the level of p-c-Met and p-STAT3.
No obvious body weight loss and no other obvious toxic signs.

Chemical Information

Molecular Weight 749.77
Formula C₄₁H₃₅N₉O₆
SMILES

O=C1NC(CCC1N(C(C2=CC(N3CCN(CC3)CCOC4=CN=C(N=C4)C5=CC=CC(CN6C(C=CC(C7=CC(C#N)=CC=C7)=N6)=O)=C5)=CC=C82)=O)C8=O)=O
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 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]. Jia C, et al. Novel Highly Potent c-Met Degraders against a Broad Range of Cancers. J Med Chem. 2025 Jul 24;68(14):15176-15197. [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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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PROTAC c-Met degrader-6

All PROTACs Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC c-Met degrader-6 Related Classifications

HY-175321 Related Classifications