2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. EGFR Btk Apoptosis
  4. Avitinib

Avitinib  (Synonyms: Abivertinib; AC0010)

Cat. No.: HY-19816 Purity: 99.90%
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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

Avitinib Chemical Structure

CAS No. : 1557267-42-1

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Based on 2 publication(s) in Google Scholar

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Avitinib Related Antibodies

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Description

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[1][2].

IC50 & Target[1]

EGFR L858R

0.18 nM (IC50)

EGFRT790M

0.18 nM (IC50)

EGFR (WT)

7.68 nM (IC50)

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.

Avitinib Related Antibodies

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.
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
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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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
References

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.

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
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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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