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AV-412

Cat. No. M3217
AV-412 Structure
Synonym:

MP-412

Size Price Availability
5mg USD 180  USD180 Custom Synthesis
10mg USD 280  USD280 Custom Synthesis
50mg USD 880  USD880 Custom Synthesis
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Quality Control & Documentation
Biological Activity

AV-412 is a second-generation, orally bioavailable dual EGFR/HER2 tyrosine kinase inhibitor. AV-412 possesses potential antineoplastic activity. AV-412 binds to and inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may result in the inhibition of tumor growth and angiogenesis, and tumor regression in EGFR/HER2-expressing tumors. AV-412 may be active against EGFR/HER2-expressing tumor cells that are resistant to first-generation kinase inhibitors. EGFR and HER2 are receptor tyrosine kinases that play major roles in tumor cell proliferation and tumor vascularization.In a study, at both 1 and 3 days following treatment, AV412-treated tumors revealed significantly more apoptotic regions compared with tumors from mice treated with vehicle alone. Furthermore, the number of carcinoma cells expressing HER2 was decreased following treatment with AV-412. AV-412 is originally developed by AVEO Pharmaceuticals, Inc. The phase I clinical trials for AV-412 has been terminated in the treatment of tumor.

Chemical Information
Molecular Weight 851.41
Formula C27H28ClFN6O.2C7H8O3S
CAS Number 451493-31-5
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Tsuyoshi Suzuki, et al. Ubiquitination and downregulation of ErbB2 and estrogen receptor-alpha by kinase inhibitor MP-412 in human breast cancer cells

[2] Karen Walker, et al. AACR-NCI-EORTC--21st International Symposium. Molecular targets and cancer therapeutics--Part 2

[3] Yinghui Zhou, et al. Chimeric mouse tumor models reveal differences in pathway activation between ERBB family- and KRAS-dependent lung adenocarcinomas

[4] Tsuyoshi Suzuki, et al. Antitumor activity of a dual epidermal growth factor receptor and ErbB2 kinase inhibitor MP-412 (AV-412) in mouse xenograft models

[5] Tsuyoshi Suzuki, et al. Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptor and ErbB2 tyrosine kinase inhibitor

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  Catalog
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Keywords: AV-412, MP-412 supplier, EGFR/HER2, inhibitors, activators


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