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

Avitinib maleate  (Synonyms: Abivertinib maleate; AC0010 maleate)

Cat. No.: HY-19816A Purity: ≥98.0%
COA Handling Instructions

Avitinib (Abivertinib) maleate 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 maleate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects.

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

Avitinib maleate Chemical Structure

Avitinib maleate Chemical Structure

CAS No. : 1557268-88-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 112 In-stock
Solution
10 mM * 1 mL in DMSO USD 112 In-stock
Solid
5 mg USD 84 In-stock
10 mg USD 144 In-stock
25 mg USD 280 In-stock
50 mg USD 450 In-stock
100 mg USD 720 In-stock
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Based on 2 publication(s) in Google Scholar

Other Forms of Avitinib maleate:

Avitinib maleate Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Avitinib (Abivertinib) maleate 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 maleate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate 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) maleate 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 maleate 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) maleate 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

603.60

Appearance

Solid

Formula

C30H30FN7O6
CAS No.
SMILES

O=C(O)/C=C\C(O)=O.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 : ≥ 100 mg/mL (165.67 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6567 mL 8.2836 mL 16.5673 mL
5 mM 0.3313 mL 1.6567 mL 3.3135 mL
10 mM 0.1657 mL 0.8284 mL 1.6567 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.14 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.14 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (4.14 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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Avitinib maleate 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.

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Keywords:

Avitinib1557268-88-8AbivertinibAC0010AC 0010AC-0010EGFRBtkApoptosisEpidermal growth factor receptorErbB-1HER1Bruton tyrosine kinaseInhibitorinhibitorinhibit

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