2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. PROTACs EGFR
  4. MS9427

MS9427 is a potent PROTAC EGFR degrader with Kds 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.

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

MS9427 Chemical Structure

MS9427 Chemical Structure

CAS No. : 2772613-37-1

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MS9427 Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

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Description

MS9427 is a potent PROTAC EGFR degrader with Kds 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].

IC50 & Target[1]

EGFR (WT)

7.1 nM (Kd)

EGFR L858R

4.3 nM (Kd)

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 EGFRDel19 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.

MS9427 Related Antibodies

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.
Molecular Weight

993.47

Formula

C48H58ClFN8O12
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0066 mL 5.0329 mL 10.0657 mL
5 mM 0.2013 mL 1.0066 mL 2.0131 mL
View the Complete Stock Solution Preparation Table

* 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.

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

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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MS9427 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MS94272772613-37-1MS 9427MS-9427PROTACsEGFREpidermal growth factor receptorErbB-1HER1anticancerantiproliferativeNSCLCUPSautophagy/lysosome pathwayInhibitorinhibitorinhibit

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