2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. WZ8040

WZ8040 

Cat. No.: HY-12029 Purity: 99.22%
COA Handling Instructions

WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits EGFR phosphorylation. WZ8040 displays 100-fold greater activity against the mutated EGFR than the normal.

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

WZ8040 Chemical Structure

WZ8040 Chemical Structure

CAS No. : 1214265-57-2

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 130 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 130 In-stock
Solid
5 mg USD 118 In-stock
10 mg USD 188 In-stock
50 mg   Get quote  
100 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

WZ8040 Related Antibodies

Top Publications Citing Use of Products

View All EGFR Isoform Specific Products:

View All Isoforms
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits EGFR phosphorylation. WZ8040 displays 100-fold greater activity against the mutated EGFR than the normal[1].

IC50 & Target

EGFR Del E746_A750

1 nM (IC50, in HCC827 cells)

EGFR Del E746_A750

6 nM (IC50, in PC9 cells)

EGFR L858R

66 nM (IC50, in H3255 cells )

EGFR L858R/T790M

9 nM (IC50, in H1975 cells)

EGFR Del E746_A750/T790M

8 nM (IC50, in PC9 GR cells)

EGFR E746_A750/MET amp

>3.3 μM (IC50, in HCC827 GR cells)

ERBB2 amp

738 nM (IC50, in H1819 cells)

ERBB2 amp

915 nM (IC50, in Calu-3 cells)

ERBB2 Ins G776V, C

744 nM (IC50, in H1781 cells)

EGFR & ERBB2 WT

1.82 μM (IC50, in HN11 cells)

In Vitro

WZ8040 exhibits IC50 values of 1 nM for HCC827 (EGFR Del E746_A750), 6 nM for PC9 (EGFR Del E746_A750), 66 nM for H3255 (EGFR L858R), 9 nM for H1975 (EGFR L858R/T790M), 8 nM for PC9 GR (EGFR Del E746_A750/T790M), >3.3 μM for HCC827 GR (EGFR E746_A750/MET amp), 738 nM for H1819 (ERBB2 amp), 915 nM for Calu-3 (ERBB2 amp), 744 nM for H1781 (ERBB2 Ins G776V, C), 1.82 μM for HN11 (EGFR & ERBB2 WT), respectively[1].

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

WZ8040 Related Antibodies

Western Blot Analysis[1]

Cell Line: NSCLC cell lines and Ba/F3 cells.
Concentration: 0-3.3 μM.
Incubation Time: 24 hours.
Result: Exhibited activity for EGFR-mutated NSCLC lines, such as HH827, PC9, H3255, H1819, Calu-3, H1781 and HN11 cells.
Molecular Weight

481.01

Appearance

Solid

Formula

C24H25ClN6OS
CAS No.
SMILES

CN1CCN(C2=CC=C(C=C2)NC3=NC=C(C(SC4=CC(NC(C=C)=O)=CC=C4)=N3)Cl)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (51.97 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0790 mL 10.3948 mL 20.7896 mL
5 mM 0.4158 mL 2.0790 mL 4.1579 mL
10 mM 0.2079 mL 1.0395 mL 2.0790 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (2.08 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1 mg/mL (2.08 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.22%

COA (244 KB) HNMR (206 KB) LCMS (264 KB)

Handling Instructions (2659 KB)
References
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WZ8040 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.

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  • Dilution Calculator

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

WZ80401214265-57-2WZ 8040WZ-8040EGFREpidermal growth factor receptorErbB-1HER1mutatedphosphorylationNSCLCInhibitorinhibitorinhibit

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