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Art. -Nr.: HY-147941

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MS9427

MS9427 is a potent PROTAC EGFR degrader with K_ds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer.
(Pink: EGFR ligand (HY-W109039); Blue: Cereblon ligand (HY-W023573); Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 95.29%
CAS. Nr.: 2772613-37-1
Formel: C₄₈H₅₈ClFN₈O₁₂
Molecular Weight:993.47

Speicherung:

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

MS9427 Chemical Structure

CAS. Nr.: 2772613-37-1

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

MS9427 is a potent PROTAC EGFR degrader with K_ds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer^[1]. (Pink: EGFR ligand (HY-W109039); Blue: Cereblon ligand (HY-W023573); Black: linker).

IC₅₀ & Target^[1]

EGFR (WT)

7.1 nM (Kd)

EGFR L858R

4.3 nM (Kd)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCC827	GI₅₀	0.87 μM Compound: 72; MS9427	Antiproliferative activity against human HCC827 cells assessed as cell growth inhibition incubated for 3 days by CCK-8 assay Antiproliferative activity against human HCC827 cells assessed as cell growth inhibition incubated for 3 days by CCK-8 assay	[PMID: 35675209]

In Vitro

MS9427 has antiproliferative activity against HCC-827 cells, with a GI₅₀ of 0.87 ± 0.27 μM^[1].
MS9427 (0-10 μM, 16 h) potently induces EGFR^Del19 degradation (DC₅₀=82 ± 73 nM) and inhibits EGFR phosphorylation (p-EGFR) in a concentration-dependent manner in HCC-827 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

HCC-827 cells
Concentration:

1, 10, 50, 100, 200, 500, 100, and 10000 nM
Incubation Time:

16 h
Result:

Inhibited EGFR phosphorylation (p-EGFR) in a concentration-dependent manner in HCC-827 cells.

Western Blot Analysis^[1]

Cell Line:

HCC-827 cells
Concentration:

100 nM
Incubation Time:

1, 2, 4, 6, 12, 24, 48 h
Result:

Induced EGFR degradation in a time-dependent manner and through the UPS and autophagy/lysosome system.

Chemical Information

CAS. Nr. 2772613-37-1
Appearance Solid
Molecular Weight 993.47
Formel C₄₈H₅₈ClFN₈O₁₂
Color Off-white to light yellow
SMILES

O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC(NCCOCCOCCOCCOCCOCCC(N4CCN(CCCOC5=CC6=C(NC7=CC=C(F)C(Cl)=C7)N=CN=C6C=C5OC)CC4)=O)=C3)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 70 mg/mL (70.46 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

1.0066 mL

5.0329 mL

10.0657 mL

5 mM

0.2013 mL

1.0066 mL

2.0131 mL

10 mM

0.1007 mL

0.5033 mL

1.0066 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)

Verweise

[1]. Yu X, et al. Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras. J Med Chem. 2022 Jun 23;65(12):8416-8443. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.0066 mL	5.0329 mL	10.0657 mL	25.1643 mL
	5 mM	0.2013 mL	1.0066 mL	2.0131 mL	5.0329 mL
	10 mM	0.1007 mL	0.5033 mL	1.0066 mL	2.5164 mL
	15 mM	0.0671 mL	0.3355 mL	0.6710 mL	1.6776 mL
	20 mM	0.0503 mL	0.2516 mL	0.5033 mL	1.2582 mL
	25 mM	0.0403 mL	0.2013 mL	0.4026 mL	1.0066 mL
	30 mM	0.0336 mL	0.1678 mL	0.3355 mL	0.8388 mL
	40 mM	0.0252 mL	0.1258 mL	0.2516 mL	0.6291 mL
	50 mM	0.0201 mL	0.1007 mL	0.2013 mL	0.5033 mL
	60 mM	0.0168 mL	0.0839 mL	0.1678 mL	0.4194 mL

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

MS9427

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MS9427 Related Classifications

HY-147941 Related Classifications

Bioz