Referencia número: HY-10346A

AV-412 free base

(Synonyms: MP-412 free base)

5 Cited Publications

Revisión del cliente

Based on 5 publication(s) in Google Scholar

AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC₅₀s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR^L858R, EGFR^T790M, EGFR^L858R/T790M and ErbB2, respectively.

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Pureza: 98.10%
No. CAS: 451492-95-8
Fòrmula: C₂₇H₂₈ClFN₆O
Peso molecular:507.00

Almacenamiento:

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

AV-412 free base Chemical Structure

No. CAS: 451492-95-8

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(In Japan)

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Bioz

Actividad biológica

Descripciòn

AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC₅₀s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR^L858R, EGFR^T790M, EGFR^L858R/T790M and ErbB2, respectively.

IC₅₀ & Target^[1]

EGFR

0.75 nM (IC₅₀)

ErbB2

19 nM (IC₅₀)

EGFR^L858R

0.51 nM (IC₅₀)

EGFR^L858R/T790M

2.3 nM (IC₅₀)

EGFR^T790M

0.79 nM (IC₅₀)

Ver todos los productos específicos de isoformas EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.1 μM Compound: 33; AV-412; MP-412	Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 72 hrs by MTS assay Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 72 hrs by MTS assay	[PMID: 28754471]

In Vitro

AV-412 inhibits autophosphorylation of EGFR and ErbB2 with IC₅₀ of 43 and 282 nM, respectively. AV-412 also inhibits epidermal growth factor (EGF)-dependent cell proliferation with an IC₅₀ of 100 nM. AV-412 abrogates EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR^[1].

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

In Vivo

In animal studies using cancer xenograft models, AV-412 (30 mg/kg) demonstrates complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively. AV-412 suppresses autophosphorylation of EGFR and ErbB2 at the dose corresponding to its antitumor efficacy. When various dosing schedules are applied, AV-412 shows significant effects with daily and every-other-day schedules, but not with a once-weekly schedule, suggesting that frequent dosing is preferable for this compound. Furthermore, AV-412 shows a significant antitumor effect on the ErbB2-overexpressing breast cancer KPL-4 cell line, which is resistant to gefitinib^[1].

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

Chemical Information

No. CAS 451492-95-8
Appearance Solid
Peso molecular 507.00
Fòrmula C₂₇H₂₈ClFN₆O
Color White to yellow
SMILES

O=C(C=C)NC1=CC2=C(NC3=CC=C(C(Cl)=C3)F)N=CN=C2C=C1C#CC(C)(C)N(CC4)CCN4C
Synonyms

MP-412 free base
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 (5)

All Flow CytometryWBOthersCell Proliferation/Viability Assay

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Journal Impact Factor

Nature

Inhibitors supercharge kinase turnover through native proteolytic circuits. [Abstract]

2026 Jan;649(8098):1032-1041. PMID: 41299171

AV-412 free base purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8098):1032-1041. [Abstract]

Immunoblot analysis of cell lines (K562 HER2WT or HER2C805S Nluc-3xFLAG reporter cell lines) treated for 15 h with AV-412 (HY-10346; 2.5 µM), neratinib (HY-32721; 10 µM), afatinib (HY-10261; 10 µM), WZ4002 (HY-12026; 10 µM).

AV-412 free base purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8098):1032-1041. [Abstract]

Luminescent reporter assay of K562 HER2WT or HER2C805S Nluc-3xFLAG reporter cell lines treated for 15 h with the indicated compounds (AV-412 (HY-10346; 2.5 µM), neratinib (HY-32721; 10 µM), afatinib (HY-10261; 10 µM), WZ4002 (HY-12026; 10 µM)) shown as normalized luminescence per genetic construct (two-way ANOVA, Sidak corrected) (n = 3).
Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Proc Natl Acad Sci U S A

Chaperone-mediated autophagy is involved in the execution of ferroptosis. [Abstract]

2019 Feb 19;116(8):2996-3005. PMID: 30718432

AV-412 free base purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2996-3005. [Abstract]

HT22 cells were pretreated with the indicated inhibitors (CDDO (Bardoxolone, HY-14909); T0070907 (HY-13202); Troglitazone (HY-50935 ); TPCA-1 (HY-10074); JAKi; STAT3i; AV-412 (HY-10346); and MK2206 (HY-10358)) and then treated with T/Z, T/S/Z, T/C/Z for 9 h or Glutamate, Erastin (T: 20 ng/ml; Z: 50 μM; S: 20 nM; C: 1 μg/ml; Glutamate: 50 mM; Erastin 10 μM) for 12 h. Cell viability was measured by CellTiterGlo assay.
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
Cancer Med

Proton pump inhibitors stabilize the expression of PD-L1 on cell membrane depending on the phosphorylation of GSK3β. [Abstract]

2024 May;13(10):e7083. PMID: 38752436

AV-412 free base purchased from MedChemExpress. Usage Cited in: Cancer Med. 2024 May;13(10):e7083. [Abstract]

FACS analysis was used to perform the MFI of cell membrane of PD‐L1 in H441 cells with control or multiply small molecular inhibitors (Seen in the Table 1, 24 h) (n = 3). AV412 (HY‐10346; 20, 50 nM), ERK1/2 inhibitor 1 (HY‐112287; 20, 50 nM), AR‐A014418 (HY‐10512; 100, 200 nM), Erlotinib (HY‐50896; 50, 100 nM).

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (98.62 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

1.9724 mL

9.8619 mL

19.7239 mL

5 mM

0.3945 mL

1.9724 mL

3.9448 mL

10 mM

0.1972 mL

0.9862 mL

1.9724 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

Concentration

Volume

Molecular Weight

Calculadora de dilución

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

Concentration _(start)

Volume _(start)

Concentration _(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 (4.93 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.

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.

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

Kinase Assay^[1]

Recombinant intracellular kinase domains of EGFR, EGFR^L858R, EGFR^T790M, EGFR^L858R/T790M, and purified EGFR from A431 cell membranes are used. Kinase reactions are carried out in 8 mM MOPS (pH 7.0), 0.2 mM ethylenediaminetetraacetic acid (EDTA), 10 mM MnCl₂, 10 mM Mg acetate, 0.1 mg/mL poly(Glu, Tyr) 4:1, [γ³³P-ATP], and 5–10 mU of enzyme, except that 250 µM of the GGMEDIYFEFMGGKKK peptide substrate is used for EGFR^T790M. Phosphorylation is initiated by the addition of ATP and is allowed to proceed for 40 min at room temperature. The reaction is stopped by the addition of 3% phosphoric acid, then aliquots of the reaction mixture are spotted onto a filtermat. After rinsing to remove peptides bound non-specifically, the filter is scintillation counted^[1].

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

Cell Assay^[1]

To test the effects of AV-412 on growth factor-dependent cell proliferation, A431 and A7r5 cells are cultured for 24 h at 37°C in the presence of 1 ng/mL epidermal growth factor and 50 ng/mL platelet-derived growth factor, respectively. The ³H-thymidine incorporation during this period is measured^[1].

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

Animal Administration^[1]

Mice: For studies examining the dosing schedule in relation to efficacy against TE-8 tumors, AV-412 is administered either once daily, every other day, or once per week for 2 weeks. Mice are killed 1 day after the final treatment, and the tumors are dissected and weighed. For evaluation of tumor phosphorylation, tumor-bearing mice are given a single administration of AV-412 and tumors are dissected 4 h later^[1].

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 (279 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Suzuki T, et al. Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptorand ErbB2 tyrosine kinase inhibitor. Cancer Sci. 2007 Dec;98(12):1977-84. [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	1.9724 mL	9.8619 mL	19.7239 mL	49.3097 mL
	5 mM	0.3945 mL	1.9724 mL	3.9448 mL	9.8619 mL
	10 mM	0.1972 mL	0.9862 mL	1.9724 mL	4.9310 mL
	15 mM	0.1315 mL	0.6575 mL	1.3149 mL	3.2873 mL
	20 mM	0.0986 mL	0.4931 mL	0.9862 mL	2.4655 mL
	25 mM	0.0789 mL	0.3945 mL	0.7890 mL	1.9724 mL
	30 mM	0.0657 mL	0.3287 mL	0.6575 mL	1.6437 mL
	40 mM	0.0493 mL	0.2465 mL	0.4931 mL	1.2327 mL
	50 mM	0.0394 mL	0.1972 mL	0.3945 mL	0.9862 mL
	60 mM	0.0329 mL	0.1644 mL	0.3287 mL	0.8218 mL
	80 mM	0.0247 mL	0.1233 mL	0.2465 mL	0.6164 mL

Keywords

AV-412 free base

5 Cited Publications

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AV-412 free base

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Publications Citing Use of MedChemExpress (MCE) AV-412 free base

Ver todos los productos específicos de isoformas EGFR

Actividad biológica

Chemical Information

Publications (5)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

AV-412 free base Related Classifications

Referencia número: HY-10346A