1. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  2. PROTACs EGFR
  3. MS154

MS154 is a first-in-class E3 ligase cereblon-recruiting EGFR degrader with Kds of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutants. MS154 potently inhibits cell proliferation in lung cancer cells.

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MS154 Chemical Structure

MS154 Chemical Structure

CAS No. : 2550393-21-8

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Description

MS154 is a first-in-class E3 ligase cereblon-recruiting EGFR degrader with Kds of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutants. MS154 potently inhibits cell proliferation in lung cancer cells[1].

IC50 & Target[1]

Cereblon

 

EGFR (WT)

1.8 nM (Kd)

EGFRL858R

3.8 nM (Kd)

Molecular Weight

901.42

Formula

C46H54ClFN8O8

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1NC(C(CC1)N2C(C3=C(C2=O)C(OCCCCCCCCNC(CCN4CCN(CCCOC5=CC6=C(NC7=CC=C(C(Cl)=C7)F)N=CN=C6C=C5OC)CC4)=O)=CC=C3)=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 : 90.14 mg/mL (100.00 mM; Need ultrasonic and warming; 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 1.1094 mL 5.5468 mL 11.0936 mL
5 mM 0.2219 mL 1.1094 mL 2.2187 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Volume (start)

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C2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.42%

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. 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 1.1094 mL 5.5468 mL 11.0936 mL 27.7340 mL
5 mM 0.2219 mL 1.1094 mL 2.2187 mL 5.5468 mL
10 mM 0.1109 mL 0.5547 mL 1.1094 mL 2.7734 mL
15 mM 0.0740 mL 0.3698 mL 0.7396 mL 1.8489 mL
20 mM 0.0555 mL 0.2773 mL 0.5547 mL 1.3867 mL
25 mM 0.0444 mL 0.2219 mL 0.4437 mL 1.1094 mL
30 mM 0.0370 mL 0.1849 mL 0.3698 mL 0.9245 mL
40 mM 0.0277 mL 0.1387 mL 0.2773 mL 0.6934 mL
50 mM 0.0222 mL 0.1109 mL 0.2219 mL 0.5547 mL
60 mM 0.0185 mL 0.0924 mL 0.1849 mL 0.4622 mL
80 mM 0.0139 mL 0.0693 mL 0.1387 mL 0.3467 mL
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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.

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Product Name:
MS154
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HY-141640
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