Cat. No.: HY-161536

PROTAC EGFR degrader 9

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Based on 1 Customer Validation

PROTAC EGFR degrader 9 (Compound C6) is an orally active CRBN-based PROTAC EGFR degrader. PROTAC EGFR degrader 9 exhibits a DC₅₀ of 10.2 nM and a K_d of 240.2 nM against EGFR^{L858R/T790M/C797S}. PROTAC EGFR degrader 9 exhibits potent degradation activity against various EGFR mutants, while sparing the EGFRWT. (Blue: CRBN ligand (HY-A0003), Black: linker (HY-161613); Pink: EGFR inhibitor (HY-161537)).
(Pink: EGFR ligand (HY-161537); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-161613)).

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

Purity: 98.35%
CAS No.: 2992670-33-2
Formula: C₄₅H₄₈F₃N₉O₆S
Molecular Weight:899.98

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

PROTAC EGFR degrader 9 Chemical Structure

CAS No.: 2992670-33-2

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Antibody-Drug Conjugates

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

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

Biological Activity

Description

PROTAC EGFR degrader 9 (Compound C6) is an orally active CRBN-based PROTAC EGFR degrader. PROTAC EGFR degrader 9 exhibits a DC₅₀ of 10.2 nM and a K_d of 240.2 nM against EGFR^{L858R/T790M/C797S}. PROTAC EGFR degrader 9 exhibits potent degradation activity against various EGFR mutants, while sparing the EGFRWT. (Blue: CRBN ligand (HY-A0003), Black: linker (HY-161613); Pink: EGFR inhibitor (HY-161537))^[1]. (Pink: EGFR ligand (HY-161537); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-161613)).

IC₅₀ & Target^[1]

Cereblon

EGFR^{L858R/T790M/C797S}

10.2 nM (DC₅₀)

EGFR^{L858R/T790M/C797S}

240.2 nM (Kd)

EGFR^{del19 T790M C797S}

36.5 nM (DC₅₀)

EGFR^L858R/T790M

88.5 nM (DC₅₀)

EGFR^del19

75.4 nM (DC₅₀)

EGFR (WT)

>300 nM (DC₅₀)

All PROTACs Isoforms :

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	97.5 nM Compound: C6	Antiproliferative activity against human A549 cells harboring wildtype EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells harboring wildtype EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 38676656]
NCI-H1975	IC₅₀	46.2 nM Compound: C6	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 38676656]
PC-9	IC₅₀	17.5 nM Compound: C6	Antiproliferative activity against human PC-9 cells harboring EGFR exon 19 deletion mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human PC-9 cells harboring EGFR exon 19 deletion mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 38676656]

In Vitro

The DC₅₀ of PROTAC EGFR degrader 9 (Compound C6) against EGFR^{Del19/T790M/C797S}, EGFR^L858R/T790M, EGFR^Del19, and EGFR^WT are 36.5, 88.5, 75.4, and >300 nM, respectively^[1].
PROTAC EGFR degrader 9 (1.2-300 nM; 24 h) degrades the EGFR^{L858R/T790M/C797S} protein in H1975-TM cells in a dose-dependent manner^[1].
PROTAC EGFR degrader 9 exhibits significant inhibitory effects on PC-9-TMb (harboring EGFR^{Del19/T790M/C797S}), H1975, PC-9, and A549 cells, with IC₅₀ values of 43.5 nM, 46.2 nM, 17.5 nM, and 97.5 nM, respectively^[1].

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

Western Blot Analysis^[1]

Cell Line:

H1975-TM cells
Concentration:

1.2 nM, 3.7 nM, 11nM, 33 nM, 100 nM, 300 nM
Incubation Time:

24 h
Result:

Degraded the EGFRL858R/T790M/C797S protein in H1975-TM cells.

Cell Cycle Analysis^[1]

Cell Line:

H1975-TM cells
Concentration:

5 nM, 10 nM, 20 nM
Incubation Time:

24 h
Result:

Arrested H1975-TM cells in the G0/G1 phase.

Apoptosis Analysis^[1]

Cell Line:

H1975-TM cells
Concentration:

33 nM, 100 nM, 300 nM
Incubation Time:

24 h
Result:

Promoted cell apoptosis.

In Vivo

PROTAC EGFR degrader 9 (Compound C6; 25-100 mg/kg; oral administration; once-daily; for 31 days) significantly reduces the level of EGFR protein in tumor tissues, inhibits EGFR phosphorylation, and blocks the activation of downstream signaling pathways^[1].

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

Animal Model:

BALB/c nude mice injected with H1975-TM^[1]
Dosage:

25 mg/kg, 100 mg/kg
Administration:

Oral administration; once-daily; for 31 days
Result:

Could effectively inhibit the NSCLC tumor growth in vivo without obvious toxicity.

Chemical Information

CAS No. 2992670-33-2
Appearance Solid
Molecular Weight 899.98
Formula C₄₅H₄₈F₃N₉O₆S
Color Light yellow to yellow
SMILES

O=C(CCCCCCN1CCN(C2=CC=C(NC3=NC=C(C(C4=CN(C5=CC=CC=C54)S(=O)(CC)=O)=N3)C(F)(F)F)C=C2)CC1)NC6=CC=CC7=C6CN(C7=O)C8C(NC(CC8)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (111.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1111 mL

5.5557 mL

11.1114 mL

5 mM

0.2222 mL

1.1111 mL

2.2223 mL

10 mM

0.1111 mL

0.5556 mL

1.1111 mL

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.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 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]. Yasheng Zhu, et al. Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting C797S Mutation. J Med Chem. 2024 May 9;67(9):7283-7300. [Content Brief]

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.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.1111 mL	5.5557 mL	11.1114 mL	27.7784 mL
	5 mM	0.2222 mL	1.1111 mL	2.2223 mL	5.5557 mL
	10 mM	0.1111 mL	0.5556 mL	1.1111 mL	2.7778 mL
	15 mM	0.0741 mL	0.3704 mL	0.7408 mL	1.8519 mL
	20 mM	0.0556 mL	0.2778 mL	0.5556 mL	1.3889 mL
	25 mM	0.0444 mL	0.2222 mL	0.4445 mL	1.1111 mL
	30 mM	0.0370 mL	0.1852 mL	0.3704 mL	0.9259 mL
	40 mM	0.0278 mL	0.1389 mL	0.2778 mL	0.6945 mL
	50 mM	0.0222 mL	0.1111 mL	0.2222 mL	0.5556 mL
	60 mM	0.0185 mL	0.0926 mL	0.1852 mL	0.4630 mL
	80 mM	0.0139 mL	0.0694 mL	0.1389 mL	0.3472 mL
	100 mM	0.0111 mL	0.0556 mL	0.1111 mL	0.2778 mL

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PROTAC EGFR degrader 9

Anti-Infection Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Orally Active Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All PROTACs Isoforms

All EGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PROTAC EGFR degrader 9 Related Classifications

Cat. No.: HY-161536