Cat. No.: HY-12001

WZ-3146

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WZ3146 is a mutant selective EGFR inhibitor with IC₅₀s of 2, 2, 5, 14 and 66 nM for EGFR^L858R, EGFR^L858R/T790M, EGFR^E746_A750, EGFR^{E746_A750/T790M} and EGFR, respectively.

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Pureté: 99.28%
CAS No.: 1214265-56-1
Formule: C₂₄H₂₅ClN₆O₂
Masse moléculaire:464.95

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

WZ-3146 Chemical Structure

CAS No.: 1214265-56-1

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

Activité biologique

Description

WZ3146 is a mutant selective EGFR inhibitor with IC₅₀s of 2, 2, 5, 14 and 66 nM for EGFR^L858R, EGFR^L858R/T790M, EGFR^E746_A750, EGFR^{E746_A750/T790M} and EGFR, respectively.

IC₅₀ & Target^[1]

EGFR^L858R

2 nM (IC₅₀)

EGFR^L858R/T790M

5 nM (IC₅₀)

EGFR^E746_A750

2 nM (IC₅₀)

EGFR^{E746_A750/T790M}

14 nM (IC₅₀)

EGFR

24 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	10 nM Compound: WZ3146	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	14 nM Compound: WZ3146	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	2 nM Compound: 4; WZ3146	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: WZ3146	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 nM Compound: WZ3146	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	2.55 μM Compound: WZ3146	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	2.74 μM Compound: WZ3146	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	24 nM Compound: 4; WZ3146	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	24 nM Compound: WZ3146	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	248 nM Compound: WZ3146	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	5 nM Compound: 4; WZ3146	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	5 nM Compound: WZ3146	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]
BaF3	IC₅₀	632 nM Compound: WZ3146	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	66 nM Compound: WZ3146	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]
Calu-3	IC₅₀	743 nM Compound: WZ3146	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	3 nM Compound: WZ3146	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	29 nM Compound: 4; WZ3146	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	29 nM Compound: WZ3146	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	73 nM Compound: WZ3146	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	0.003 μM Compound: 3h	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	EC₅₀	0.015 μM Compound: 3h	Antiproliferative activity against EGFR-deficient human PC9 cells Antiproliferative activity against EGFR-deficient human PC9 cells	[PMID: 21208802]
PC-9	IC₅₀	15 nM Compound: WZ3146	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

WZ3146 is a novel EGFR inhibitor, suppresses the growth of EGFR T790M containing cell lines and inhibits EGFR phosphorylation^[1].

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

Chemical Information

CAS No. 1214265-56-1
Appearance Solid
Masse moléculaire 464.95
Formule C₂₄H₂₅ClN₆O₂
Color White to off-white
SMILES

CN1CCN(C2=CC=C(C=C2)NC3=NC=C(C(OC4=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	2 years
	-20°C	1 year

Solvant et solubilité

In Vitro:

DMSO : 62.5 mg/mL (134.42 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

2.1508 mL

10.7538 mL

21.5077 mL

5 mM

0.4302 mL

2.1508 mL

4.3015 mL

10 mM

0.2151 mL

1.0754 mL

2.1508 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: ≥ 2.5 mg/mL (5.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, 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

Protocole

Kinase Assay^[1]

In vitro inhibitory enzyme kinetic assays are carried out in triplicate using the ATP/NADH coupled assay system in a 96-well format. The final reaction mixture contains 0.5mg/mL Bovine Serum Albumin (BSA), 2mM MnCl₂, 1mM phospho(enol) pyruvic acid, 1mM TCEP, 0.1M Hepes 7.4, 2.5mM poly-[Glu4Tyr1] peptide, 1/50 of the final reaction mixture volume of pyruvate kinase/lactic dehydrogenase enzymes from rabbit muscle, 0.5mM NADH, 0.5μM EGFR kinase, 100μM ATP and varied amount of inhibitors. Inhibitors and ATP are mixed and made separate stock from the mixture with all other ingredients and added last to the latter to start the reaction. Steady state initial velocity data are drawn from the slopes of the A340 curves^[1].

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

Animal Administration^[1]

Growth and inhibition of growth is assessed by MTS assay. Ba/F3 cells are exposed to WZ3146 treatment for 72 hours. Growth and inhibition of growth is assessed by MTS assay^[1].

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (271 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1508 mL	10.7538 mL	21.5077 mL	53.7692 mL
	5 mM	0.4302 mL	2.1508 mL	4.3015 mL	10.7538 mL
	10 mM	0.2151 mL	1.0754 mL	2.1508 mL	5.3769 mL
	15 mM	0.1434 mL	0.7169 mL	1.4338 mL	3.5846 mL
	20 mM	0.1075 mL	0.5377 mL	1.0754 mL	2.6885 mL
	25 mM	0.0860 mL	0.4302 mL	0.8603 mL	2.1508 mL
	30 mM	0.0717 mL	0.3585 mL	0.7169 mL	1.7923 mL
	40 mM	0.0538 mL	0.2688 mL	0.5377 mL	1.3442 mL
	50 mM	0.0430 mL	0.2151 mL	0.4302 mL	1.0754 mL
	60 mM	0.0358 mL	0.1792 mL	0.3585 mL	0.8962 mL
	80 mM	0.0269 mL	0.1344 mL	0.2688 mL	0.6721 mL
	100 mM	0.0215 mL	0.1075 mL	0.2151 mL	0.5377 mL

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WZ-3146

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Voir tous les produits spécifiques à Isoform EGFR

Activité biologique

Chemical Information

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

WZ-3146 Related Classifications

HY-12001 Related Classifications