1. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  2. PROTACs EGFR Apoptosis
  3. PROTAC EGFR degrader 7

PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research. PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

PROTAC EGFR degrader 7 Chemical Structure

PROTAC EGFR degrader 7 Chemical Structure

Size Price Stock Quantity
1 mg USD 250 In-stock
5 mg USD 750 In-stock
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50 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research[1]. PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

EGFRL858R/T790M

13.2 nM (DC50)

In Vivo

PROTAC EGFR degrader 7 (compound 13b) (BALB/c mice bearing NCI–H1975 cells, 10 mg/kg, IP, once a day for 24 days) effectively and selectively inhibits NCI–H1975 xenograft tumor growth, with the tumor growth inhibition (TGI%) of 63.7%[1].

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

Molecular Weight

836.94

Formula

C46H48N10O6

Appearance

Solid

Color

Light yellow to yellow

SMILES

C#CCN(CCN(C1=CC(OC)=C(C=C1NC(C=C)=O)NC2=NC(C3=CN(C4=CC=CC=C34)C)=CC=N2)C)CCCC(NC5=C6CN(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 120 mg/mL (143.38 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 1.1948 mL 5.9741 mL 11.9483 mL
5 mM 0.2390 mL 1.1948 mL 2.3897 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
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 (sealed storage, away from moisture and light). 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 1.1948 mL 5.9741 mL 11.9483 mL 29.8707 mL
5 mM 0.2390 mL 1.1948 mL 2.3897 mL 5.9741 mL
10 mM 0.1195 mL 0.5974 mL 1.1948 mL 2.9871 mL
15 mM 0.0797 mL 0.3983 mL 0.7966 mL 1.9914 mL
20 mM 0.0597 mL 0.2987 mL 0.5974 mL 1.4935 mL
25 mM 0.0478 mL 0.2390 mL 0.4779 mL 1.1948 mL
30 mM 0.0398 mL 0.1991 mL 0.3983 mL 0.9957 mL
40 mM 0.0299 mL 0.1494 mL 0.2987 mL 0.7468 mL
50 mM 0.0239 mL 0.1195 mL 0.2390 mL 0.5974 mL
60 mM 0.0199 mL 0.0996 mL 0.1991 mL 0.4978 mL
80 mM 0.0149 mL 0.0747 mL 0.1494 mL 0.3734 mL
100 mM 0.0119 mL 0.0597 mL 0.1195 mL 0.2987 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:
PROTAC EGFR degrader 7
Cat. No.:
HY-147858
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