Cat. No.: HY-12029

WZ8040

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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.

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Pureté: 98.29%
CAS No.: 1214265-57-2
Formule: C₂₄H₂₅ClN₆OS
Masse moléculaire:481.01

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

WZ8040 Chemical Structure

CAS No.: 1214265-57-2

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Antibody-Drug Conjugates

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

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)

Voir tous les produits spécifiques à Isoform EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	2 nM Compound: 5; WZ8040	Antiproliferative activity against gefitinib sensitive mouse BA/F3 cells expressing EGFR exon 19 del E746_A750 activating mutant after 72 hrs by MTS assay Antiproliferative activity against gefitinib sensitive mouse BA/F3 cells expressing EGFR exon 19 del E746_A750 activating mutant after 72 hrs by MTS assay	[PMID: 26882288]
BaF3	IC₅₀	2 nM Compound: WZ8040	Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	2.01 μM Compound: WZ8040	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	2.54 μM Compound: WZ8040	Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	20 nM Compound: WZ8040	Antiproliferative activity against mouse BaF3 cells harboring ERBB2 Ins G776V,C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring ERBB2 Ins G776V,C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	306 nM Compound: WZ8040	Antiproliferative activity against mouse BaF3 cells harboring EGFR A767_V769dupASV mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR A767_V769dupASV mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	32 nM Compound: 5; WZ8040	Antiproliferative activity against mouse BA/F3 cells expressing wild type EGFR after 72 hrs by MTS assay Antiproliferative activity against mouse BA/F3 cells expressing wild type EGFR after 72 hrs by MTS assay	[PMID: 26882288]
BaF3	IC₅₀	32 nM Compound: WZ8040	Antiproliferative activity against mouse BaF3 cells harboring wildtype ERBB2 assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring wildtype ERBB2 assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	374 nM Compound: WZ8040	Antiproliferative activity against mouse BaF3 cells harboring ERBB2 Ins 774YVMA mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring ERBB2 Ins 774YVMA mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	48 nM Compound: WZ8040	Antiproliferative activity against mouse BaF3 cells harboring EGFR vIII mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR vIII mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	6 nM Compound: WZ8040	Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	6 nM Compound: WZ8040	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	9 nM Compound: 5; WZ8040	Antiproliferative activity against gefitinib resistant mouse BA/F3 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTS assay Antiproliferative activity against gefitinib resistant mouse BA/F3 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTS assay	[PMID: 26882288]
BaF3	IC₅₀	9 nM Compound: WZ8040	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
Calu-3	IC₅₀	915 nM Compound: WZ8040	Antiproliferative activity against human Calu-3 cells harboring ERBB2 amp mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human Calu-3 cells harboring ERBB2 amp mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
HCC827	IC₅₀	1 nM Compound: WZ8040	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
NCI-H1975	IC₅₀	9 nM Compound: 5; WZ8040	Antiproliferative activity against gefitinib resistant human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTS assay Antiproliferative activity against gefitinib resistant human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTS assay	[PMID: 26882288]
NCI-H1975	IC₅₀	9 nM Compound: WZ8040	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
NCI-H3255	IC₅₀	66 nM Compound: WZ8040	Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
PC-9	EC₅₀	0.006 μM Compound: 4b	Antiproliferative activity against EGFR-deficient human PC9 cells Antiproliferative activity against EGFR-deficient human PC9 cells	[PMID: 21208802]
PC-9	EC₅₀	0.008 μM Compound: 4b	Antiproliferative activity against growth-resistant human PC9 cells expressing EGFR E746_A750/T790M mutant Antiproliferative activity against growth-resistant human PC9 cells expressing EGFR E746_A750/T790M mutant	[PMID: 21208802]
PC-9	IC₅₀	6 nM Compound: WZ8040	Antiproliferative activity against human PC-9 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human PC-9 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]

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].

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

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.

Chemical Information

CAS No. 1214265-57-2
Appearance Solid
Masse moléculaire 481.01
Formule C₂₄H₂₅ClN₆OS
Color Light yellow to green yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

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

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. 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (271 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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)
Instruction de manipulation (2659 KB)

Références

[1]. Zhou W, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4. [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

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	2.0790 mL	10.3948 mL	20.7896 mL	51.9740 mL
	5 mM	0.4158 mL	2.0790 mL	4.1579 mL	10.3948 mL
	10 mM	0.2079 mL	1.0395 mL	2.0790 mL	5.1974 mL
	15 mM	0.1386 mL	0.6930 mL	1.3860 mL	3.4649 mL
	20 mM	0.1039 mL	0.5197 mL	1.0395 mL	2.5987 mL
	25 mM	0.0832 mL	0.4158 mL	0.8316 mL	2.0790 mL
	30 mM	0.0693 mL	0.3465 mL	0.6930 mL	1.7325 mL
	40 mM	0.0520 mL	0.2599 mL	0.5197 mL	1.2993 mL
	50 mM	0.0416 mL	0.2079 mL	0.4158 mL	1.0395 mL

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WZ8040

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Voir tous les produits spécifiques à Isoform EGFR

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

WZ8040 Related Classifications

Cat. No.: HY-12029