Cat. No.: HY-19816

Avitinib

(Synonyms: Abivertinib; AC0010)

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

Avitinib (Abivertinib) is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC₅₀ values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib shows anticancer effects.

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

Purity: 99.95%
CAS No.: 1557267-42-1
Formula: C₂₆H₂₆FN₇O₂
Molecular Weight:487.53

Storage:

4°C, sealed storage, away from moisture

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

Avitinib Chemical Structure

CAS No.: 1557267-42-1

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Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

EGFR L858R

0.18 nM (IC₅₀)

EGFR^T790M

0.18 nM (IC₅₀)

EGFR (WT)

7.68 nM (IC₅₀)

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	1.92 μM Compound: 12b	Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability measured after 48 hrs by CCK8 assay Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability measured after 48 hrs by CCK8 assay	[PMID: 34315040]
BEAS-2B	IC₅₀	3.68 μM Compound: 12b	Cytotoxicity against human BEAS-2B cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay Cytotoxicity against human BEAS-2B cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay	[PMID: 34315040]
HCC827	IC₅₀	0.1 μM Compound: 12b	Cytotoxicity against human HCC827 cells harboring EGFR del E746-A750 mutant assessed as reduction in cell viability measured after 48 hrs by CCK8 assay Cytotoxicity against human HCC827 cells harboring EGFR del E746-A750 mutant assessed as reduction in cell viability measured after 48 hrs by CCK8 assay	[PMID: 34315040]
NCI-H1975	IC₅₀	1.56 μM Compound: 12b	Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 48 hrs by CCK8 assay Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 48 hrs by CCK8 assay	[PMID: 34315040]
NCI-H460	IC₅₀	6.02 μM Compound: 12b	Cytotoxicity against human NCI-H460 cells harboring wild type EGFR assessed as reduction in cell viability measured after 48 hrs by CCK8 assay Cytotoxicity against human NCI-H460 cells harboring wild type EGFR assessed as reduction in cell viability measured after 48 hrs by CCK8 assay	[PMID: 34315040]

In Vitro

Avitinib (AC0010; 0.13 nM-2 μM; 2 h) selectively inhibits mutant EGFR phosphorylation with IC₅₀ values of 7.3 and 2.8 nM in NCI-H1975 and NIH/3T3_TC32T8 cells, about 115- and 298-fold more sensitive than that of the inhibition of wild-type EGFR in A431. Avitinib potently inhibits EGFR-Tyr1068 phosphorylation in NCI-H1975 cells, and the selectivity ratio is at 65-fold for NCI-H1975 cells versus A431 cells. In addition to inhibition of EGFR-Tyr1068 phosphorylation, Avitinib inhibits phosphorylation of the downstream targets Akt and ERK1/2 in NCI-H1975 and HCC827 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

NCI-H1975, HCC827, A431 cells
Concentration:

0.13 nM, 0.64 nM, 3.2 nM, 16 nM, 80 nM, 0.4 μM, 2 μM
Incubation Time:

2 h
Result:

Selectively inhibits mutant EGFR phosphorylation with IC50 values of 7.3 and 2.8 nM in NCI-H1975 and NIH/3T3_TC32T8 cells.

In Vivo

Avitinib (AC0010; 12.5-500 mg/kg; orally administration; once daily; for 14 days) inhibits EGFR-mutant tumor growth but not wild-type EGFR tumor growth in xenograft models over extended duration^[1].

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

Animal Model:

Nu/Nu nude mice (Six- to 8-week-old) injected with NCI-H1975 and A431 cells^[1]
Dosage:

12.5, 50, and 500 mg/kg
Administration:

Orally administration; once daily; for 14 days
Result:

Inhibited EGFR-mutant tumor growth but not wild-type EGFR tumor growth.

Chemical Information

CAS No. 1557267-42-1
Appearance Solid
Molecular Weight 487.53
Formula C₂₆H₂₆FN₇O₂
Color White to off-white
SMILES

O=C(C=C)NC1=CC=CC(OC2=NC(NC3=CC(F)=C(N4CCN(C)CC4)C=C3)=NC5=C2C=CN5)=C1
Synonyms

Abivertinib; AC0010
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Publications (3)

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Journal Impact Factor

Bioorg Chem

Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]

2024 Jun:147:107412. PMID: 38696845
Molecules

A Validated LC-MS/MS Assay for the Simultaneous Quantification of the FDA-Approved Anticancer Mixture (Encorafenib and Binimetinib): Metabolic Stability Estimation. [Abstract]

2021 May 5;26(9):2717. PMID: 34063139
J Pharm Biomed Anal

Reactive intermediates and bioactivation pathways characterization of avitinib by LC-MS/MS: In vitro metabolic investigation. [Abstract]

2019 Feb 5:164:659-667. PMID: 30472584

Solvent & Solubility

In Vitro:

DMSO : 83.33 mg/mL (170.92 mM; Need ultrasonic; 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

2.0512 mL

10.2558 mL

20.5116 mL

5 mM

0.4102 mL

2.0512 mL

4.1023 mL

10 mM

0.2051 mL

1.0256 mL

2.0512 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

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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: ≥ 3.57 mg/mL (7.32 mM); Clear solution

This protocol yields a clear solution of ≥ 3.57 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.7 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% Corn Oil

Solubility: ≥ 3.57 mg/mL (7.32 mM); Clear solution

This protocol yields a clear solution of ≥ 3.57 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 (35.7 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 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)
- 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)
Handling Instructions (2659 KB)

References

[1]. Xu X, Mao L, Xu W, et al. AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients. Mol Cancer Ther. 2016;15(11):2586-2597. [Content Brief]

[2]. Yan X, Zhou Y, Huang S, et al. Promising efficacy of novel BTK inhibitor AC0010 in mantle cell lymphoma. J Cancer Res Clin Oncol. 2018;144(4):697-706. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0512 mL	10.2558 mL	20.5116 mL	51.2789 mL
	5 mM	0.4102 mL	2.0512 mL	4.1023 mL	10.2558 mL
	10 mM	0.2051 mL	1.0256 mL	2.0512 mL	5.1279 mL
	15 mM	0.1367 mL	0.6837 mL	1.3674 mL	3.4186 mL
	20 mM	0.1026 mL	0.5128 mL	1.0256 mL	2.5639 mL
	25 mM	0.0820 mL	0.4102 mL	0.8205 mL	2.0512 mL
	30 mM	0.0684 mL	0.3419 mL	0.6837 mL	1.7093 mL
	40 mM	0.0513 mL	0.2564 mL	0.5128 mL	1.2820 mL
	50 mM	0.0410 mL	0.2051 mL	0.4102 mL	1.0256 mL
	60 mM	0.0342 mL	0.1709 mL	0.3419 mL	0.8546 mL
	80 mM	0.0256 mL	0.1282 mL	0.2564 mL	0.6410 mL
	100 mM	0.0205 mL	0.1026 mL	0.2051 mL	0.5128 mL

Keywords

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Avitinib

Apoptosis Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Differentiation Inducing Compound Library

Orally Active Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cysteine Targeted Covalent Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Avitinib

All EGFR Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Avitinib Related Classifications

Cat. No.: HY-19816