1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR

AV-412 free base (Synonyms: MP-412 free base)

Cat. No.: HY-10346A Purity: 98.49%
Handling Instructions

AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.

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

AV-412 free base Chemical Structure

AV-412 free base Chemical Structure

CAS No. : 451492-95-8

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

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  • References

Description

AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.

IC50 & Target[1]

EGFR

0.75 nM (IC50)

ErbB2

19 nM (IC50)

EGFRL858R

0.51 nM (IC50)

EGFRL858R/T790M

2.3 nM (IC50)

EGFRT790M

0.79 nM (IC50)

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].

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (98.62 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
References
Kinase Assay
[1]

Recombinant intracellular kinase domains of EGFR, EGFRL858R, EGFRT790M, EGFRL858R/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 EGFRT790M. 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].

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].

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].

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

References
Molecular Weight

507.00

Formula

C₂₇H₂₈ClFN₆O

CAS No.

451492-95-8

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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AV-412 free base
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HY-10346A
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AV-412 free base

Cat. No.: HY-10346A