Avitinib (Synonyms: Abivertinib; AC0010)

Name: Avitinib
Brand: MedChemExpress
SKU: HY-19816
Rating: 5.0 (3 reviews)

Cat. No.: HY-19816 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

Avitinib Chemical Structure

CAS No. : 1557267-42-1

Size	Price	Stock	Quantity
5 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Avitinib:

Avitinib maleate In-stock

3 Publications Citing Use of MCE Avitinib

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

EGFR L858R

0.18 nM (IC₅₀)

EGFR^T790M

0.18 nM (IC₅₀)

EGFR (WT)

7.68 nM (IC₅₀)

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.

Clinical Trial

Molecular Weight

487.53

Formula

C₂₆H₂₆FN₇O₂

CAS No.

1557267-42-1

Appearance

Solid

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

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)

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (256.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

COA (248 KB) HNMR (195 KB) LCMS (92 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]

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

Avitinib 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.

Keywords:

Avitinib1557267-42-1Abivertinib AC0010AC0010AC 0010AC-0010EGFRBtkApoptosisEpidermal growth factor receptorErbB-1HER1Bruton tyrosine kinaseInhibitorinhibitorinhibit

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Avitinib (Synonyms: Abivertinib; AC0010)

Customer Review

Other Forms of Avitinib:

Avitinib Related Antibodies

3 Publications Citing Use of MCE Avitinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Avitinib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Avitinib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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