Referencia número: HY-18750

Zorifertinib

(Synonyms: AZD3759)

7 Cited Publications

Revisión del cliente

Based on 7 publication(s) in Google Scholar

Zorifertinib (AZD3759) is a potent, orally active, BBB-penetrant, EGFR inhibitor. At K_m ATP concentrations, the IC₅₀s are 0.3, 0.2, and 0.2 nM for EGFR^wt, EGFR^L858R, and EGFR^{exon 19Del}, respectively. Zorifertinib induces cancer cell apoptosis. Zorifertinib has antitumor activity, and can be used for NSCLC, HCC etc. research.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.37%
No. CAS: 1626387-80-1
Fòrmula: C₂₂H₂₃ClFN₅O₃
Peso molecular:459.90

Almacenamiento:

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

Zorifertinib Chemical Structure

No. CAS: 1626387-80-1

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (7)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

EGFR

0.3 nM (IC₅₀)

EGFR^L858R

0.2 nM (IC₅₀)

EGFR^{Exon 19 deletion}

0.2 nM (IC₅₀)

Ver todos los productos específicos de isoformas EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	3.5 μM Compound: AZD3759	Antiproliferative activity against human A431 cells after 72 hrs by MTT assay Antiproliferative activity against human A431 cells after 72 hrs by MTT assay	[PMID: 30195240]
A549	IC₅₀	28.67 μM Compound: 2; AZD3759	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 30655941]
BEAS-2B	IC₅₀	18.66 μM Compound: AZD3759	Cytotoxicity against human BEAS2B cells after 72 hrs by MTT assay Cytotoxicity against human BEAS2B cells after 72 hrs by MTT assay	[PMID: 30195240]
HCC827	IC₅₀	0.03 μM Compound: AZD3759	Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay	[PMID: 30195240]
NCI-H1975	IC₅₀	24.16 μM Compound: AZD3759	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay	[PMID: 30195240]
NCI-H3255	IC₅₀	0.09 μM Compound: AZD3759	Antiproliferative activity against human H3255 cells after 72 hrs by MTT assay Antiproliferative activity against human H3255 cells after 72 hrs by MTT assay	[PMID: 30195240]
NCI-H3255	IC₅₀	7 nM Compound: 1m, AZD3759	Antiproliferative against human H3255 cells expressing EGFR L858R mutant after 72 hrs by MTS assay Antiproliferative against human H3255 cells expressing EGFR L858R mutant after 72 hrs by MTS assay	[PMID: 26313252]
NCI-H838	IC₅₀	21556 nM Compound: 1m, AZD3759	Antiproliferative against human NCI-H838 cells expressing EGFR wild-type after 72 hrs by MTS assay Antiproliferative against human NCI-H838 cells expressing EGFR wild-type after 72 hrs by MTS assay	[PMID: 26313252]
PC-9	IC₅₀	0.05 μM Compound: AZD3759	Antiproliferative activity against human PC9 cells after 72 hrs by MTT assay Antiproliferative activity against human PC9 cells after 72 hrs by MTT assay	[PMID: 30195240]
PC-9	IC₅₀	7.4 nM Compound: 1m, AZD3759	Inhibition of EGFR exon19 deletion mutant phosphorylation in human PC9 cells Inhibition of EGFR exon19 deletion mutant phosphorylation in human PC9 cells	[PMID: 26313252]
PC-9	IC₅₀	7.7 nM Compound: 1m, AZD3759	Antiproliferative against human PC9 cells expressing EGFR exon19 deletion mutant after 72 hrs by MTS assay Antiproliferative against human PC9 cells expressing EGFR exon19 deletion mutant after 72 hrs by MTS assay	[PMID: 26313252]

In Vitro

At 2 mM of ATP concentrations, the IC₅₀s are 102, 7.6, and 2.4 nM for EGFR^wt, EGFR^L858R, and EGFR^{exon 19Del}, respectively. Zorifertinib (AZD3759) also inhibits pEGFR in H838^wt, H3255^L858R, and PC-9^{exon 19Del} with IC₅₀ of 64.5, 7.2, and 7.4 nM, respectively. In cellular phosphorylation studies, Zorifertinib also demonstrates 9-fold inhibition selectivity in EGFR-activating mutant cell lines over EGFR wild-type cell lines (H838 cell line)^[1].

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

In Vivo

Following oral dosing in rats at 2 mg/kg, absorption of Zorifertinib (AZD3759) is rapid with blood C_max of 0.58 μM achieved at 1.0 h. Subsequently, blood concentrations of Zorifertinib decline monoexponentially with a mean elimination half-life of 4.3 h, which is close to the same parameter obtained from intravenous dosing of 4.1 h. The bioavailability following an oral dose in rats is 91%. Blood pharmacokinetic parameters of Zorifertinib in male dogs are determined following both a single dose intravenous infusion and oral administration. Following the IV dose in dogs, Zorifertinib blood clearance is determined as 14 mL/min per kg, and the volume of distribution is 6.4 L/kg. Its elimination half-life is 6.2 h. Absorption of Zorifertinib is rapid with blood C_max (698 nM) occurring between 0.5 and 1.5 h. The oral bioavailability of Zorifertinib is excellent at 90%. Zorifertinib demonstrated significant dose-dependent antitumor efficacy (78% tumor growth inhibition at 7.5 mg/kg qd and tumor regression at 15 mg/kg qd, respectively, 4 weeks after treatment) with <20% body weight loss, whereas CP-358774 has a limited effect in this model. At the end of the study, brain tissues are collected for histological assessment. Significantly decreased tumor area is observed by Zorifertinib treatment at the doses of 7.5 and 15 mg/kg. In addition, modulation of pEGFR is detected by a single dose of Zorifertinib at 15 mg/kg 1h after dosing, which confirmed target engagement by Zorifertinib^[1].

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

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1626387-80-1
Appearance Solid
Peso molecular 459.90
Fòrmula C₂₂H₂₃ClFN₅O₃
Color White to off-white
SMILES

ClC1=CC=CC(NC2=NC=NC3=CC(OC)=C(OC(N4[C@H](C)CN(C)CC4)=O)C=C23)=C1F
Synonyms

AZD3759
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (7)

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Journal Impact Factor

Nat Commun

Supporting cells orchestrate noise-induced hearing loss via a Gasdermin D-dependent signaling loop with hair cells. [Abstract]

2025 Dec 17;16(1):11181. PMID: 41407982
Sci Adv

In silico transcriptome screens identify epidermal growth factor receptor inhibitors as therapeutics for noise-induced hearing loss. [Abstract]

Sci Adv. 2024 Jun 21;10(25):eadk2299. d PMID: 38896614
RSC Adv

Profiling of in vivo, in vitro and reactive zorifertinib metabolites using liquid chromatography ion trap mass spectrometry. [Abstract]

2022 Jul 21;12(32):20991-21003. PMID: 35919181
J Neurochem

Molecular prognostic of nine parthanatos death-related genes in glioma, particularly in COL8A1 identification. [Abstract]

2024 Mar;168(3):205-223. PMID: 38225203
J Pharm Biomed Anal

Estimation of zorifertinib metabolic stability in human liver microsomes using LC-MS/MS. [Abstract]

2022 Mar 20:211:114626. PMID: 35123331
bioRxiv

In Silico Transcriptome-based Screens Identify Epidermal Growth Factor Receptor Inhibitors as Therapeutics for Noise-induced Hearing Loss. [Abstract]

2023 Jun 9:2023.06.07.544128. PMID: 37333346
Patent

US20220177473A1.

Solvente y solubilidad

In Vitro:

DMSO : ≥ 50 mg/mL (108.72 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.1744 mL

10.8719 mL

21.7439 mL

5 mM

0.4349 mL

2.1744 mL

4.3488 mL

10 mM

0.2174 mL

1.0872 mL

2.1744 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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 (5.44 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 (5.44 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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 (5.44 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.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution

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

Protocolo

Cell Assay^[1]

Cell proliferation assay is determined by MTS methods. Briefly, cells are seeded in 96-well plates (at a density to allow for logarithmic growth during the 72-hour assay) and incubated overnight at 37°C and 5% CO₂. Cells are then exposed to concentrations of compounds (e.g., Zorifertinib) ranging from 30 mM to 0.3μM for 72 hours. For the MTS endpoint, cell proliferation is measured by the CellTiter AQueous Non-Radioactive Cell Proliferation Assay reagent. Absorbance is measured with a Tecan Ultra instrument. Predose measurements are made, and concentration needed to reduce the growth of treated cells to half that of untreated cells (GI₅₀) values are determined using absorbance readings^[1].

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

Animal Administration^[1]

Rats^[1]
Male Han Wistar rats are orally dosed with the Zorifertinib at 2 mg/kg in 1% methylcellulose. At 0.25, 0.5, 1, 2, 4 and 7 hour post-dose, cerebral spinal fluid (CSF) is collected from cisterna magna, and blood samples (>60 μL/time point/each site) are collected via cardiac puncture, into separate EDTA coagulated tubes, and then immediately diluted with 3-fold volume of water. Brain tissue is harvested and homogenized in 3x volume of 100 mM phosphate buffered saline (pH7.4). All samples are stored at -70°C prior to LC/MS/MS analysis.

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (282 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Zeng Q, et al. Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. J Med Chem. 2015 Oct 22;58(20):8200-15. [Content Brief]

[2]. Chao D, et al. AZD3759 induces apoptosis in hepatoma cells by activating a p53-SMAD4 positive feedback loop. Biochem Biophys Res Commun. 2019 Feb 5;509(2):535-540. [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	2.1744 mL	10.8719 mL	21.7439 mL	54.3596 mL
	5 mM	0.4349 mL	2.1744 mL	4.3488 mL	10.8719 mL
	10 mM	0.2174 mL	1.0872 mL	2.1744 mL	5.4360 mL
	15 mM	0.1450 mL	0.7248 mL	1.4496 mL	3.6240 mL
	20 mM	0.1087 mL	0.5436 mL	1.0872 mL	2.7180 mL
	25 mM	0.0870 mL	0.4349 mL	0.8698 mL	2.1744 mL
	30 mM	0.0725 mL	0.3624 mL	0.7248 mL	1.8120 mL
	40 mM	0.0544 mL	0.2718 mL	0.5436 mL	1.3590 mL
	50 mM	0.0435 mL	0.2174 mL	0.4349 mL	1.0872 mL
	60 mM	0.0362 mL	0.1812 mL	0.3624 mL	0.9060 mL
	80 mM	0.0272 mL	0.1359 mL	0.2718 mL	0.6795 mL
	100 mM	0.0217 mL	0.1087 mL	0.2174 mL	0.5436 mL

Keywords

Zorifertinib

7 Cited Publications

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Zorifertinib

Anti-Infection Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

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Publications Citing Use of MedChemExpress (MCE) Zorifertinib

Ver todos los productos específicos de isoformas EGFR

Actividad biológica

Chemical Information

Publications (7)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Zorifertinib Related Classifications

HY-18750 Related Classifications