SYN-1012-M0011 mgCHF 270.00
SYN-1012-M0055 mgCHF 546.00
SYN-1012-M01010 mgCHF 858.00
|Solubility||Soluble in DMSO or ethanol.|
|Declaration||Manufactured by SynKinase.|
|Other Product Data||
Target: EGFR | Kinase Group: RTK | Substrate: Tyrosine
Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
|Use/Stability||Stable for at least 2 years after receipt when stored at -20°C.|
|Product Specification Sheet|
AV-412 is a potent dual inhibitor of EGFR and ErbB2 tyrosine kinases, including the mutant EGFR(L858R,T790M), which is clinically resistant to the EGFR-specific kinase inhibitors erlotinib and gefitinib. In enzyme assays assay the compound inhibited the EGFR variants and ErbB2 in the nanomolar range with over 100-fold selectivity compared with other kinases, apart from ABL and FLT1, which were both moderately sensitive to the compound. In cells, AV-412 inhibited autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively. It also inhibited epidermal growth factor (EGF)-dependent cell proliferation with an IC(50) of 100nM. Moreover, AV-412 abrogated EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. In animal studies using cancer xenograft models, AV-412 (30mg/kg) demonstrated complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively.
- Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptor and ErbB2 tyrosine kinase inhibitor: T. Suzuki, et al.; Cancer Sci. 98, 1977 (2007)