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AV-412 free base

Catalog No. TQ0293   CAS 451492-95-8
Synonyms: MP-412 free base

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

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AV-412 free base Chemical Structure
AV-412 free base, CAS 451492-95-8
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2 mg 5 days $ 66.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AV-412 free base is an EGFR inhibitor (IC50s: 0.75, 0.79, 0.5, 2.3, 19 nM for EGFR, EGFR(T790M), EGFR(L858R), EGFR(L858R/T790M) and ErbB2).
Targets&IC50 EGFR:0.75 nM, EGFR (L858R):0.51 nM, EGFR (T790M):0.79 nM, EGFR (L858R/T790M):2.3 nM, ErbB2:19 nM
In vitro AV-412 inhibits autophosphorylation of EGFR and ErbB2 (IC50: 43 and 282 nM). AV-412 also inhibits EGF-dependent cell proliferation (IC50: 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.
In vivo In cancer xenograft models, AV-412 (30 mg/kg) effectively halts the growth of A431 and BT-474 cell lines, which notably overexpress EGFR and ErbB2, respectively. This compound also inhibits autophosphorylation of EGFR and ErbB2, correlating with its antitumor properties. AV-412 exhibits considerable antitumor activity across different dosing regimens, displaying significant efficacy with daily and every-other-day administrations, but not with once-weekly dosing. Additionally, it significantly combats the gefitinib-resistant, ErbB2-overexpressing breast cancer cell line KPL-4, affirming its potent antitumor effects.
Kinase Assay 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 filter mat. After rinsing to remove peptides bound non-specifically, the filter is scintillation counted.
Cell Research 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.
Animal Research 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.
Synonyms MP-412 free base
Molecular Weight 507
Formula C27H28ClFN6O
CAS No. 451492-95-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 48 mg/mL (94.68 mM)

TargetMolReferences and Literature

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.

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Keywords

AV-412 free base 451492-95-8 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR MP 412 AV 412 AV412 free base AV 412 free base MP-412 MP-412 free base MP412 AV-412 AV412 inhibitor inhibit

 

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