| Name | BMS-599626 Hydrochloride |
| Description | BMS-599626 Hydrochloride (AC480 Hydrochloride) is an orally bioavailable inhibitor of the HER1, HER2, and HER4 tyrosine kinases (IC50 = 22, 32, and 190 nM, respectively) with potential antineoplastic activity, inhibiting the proliferation of tumor cells that overexpress these receptors. |
| In vitro | BMS-599626 Hydrochloride abrogates HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC50s in the range of 0.24 to 1 μM.In GEO cells, HER1 phosphorylation is stimulated by treatment with EGF and is inhibited by BMS-599626 Hydrochloride (IC50=0. 75 μM).There is also nearly complete inhibition of EGF-dependent MAPK (0. 8 μM) but only partial inhibition of AKT signaling.The latter likely reflects the activation of AKT by multiple upstream signals.Treatment of N87 cells with BMS-599626 Hydrochloride leads to the inhibition of HER2 (0. 38 μM), which is expressed to a high level because of gene amplification, as well as MAPK and AKT phosphorylation (0.35 μM for both) [1]. |
| In vivo | BMS-599626 Hydrochloride given before and during irradiation improved the radioresponse of HN5 tumors in vivo [2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 90.0 mg/mL (158.7 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (5.82 mM), Sonication is recommended.
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| Keywords | HER4 | HER2 | HER1 | BMS-599626 Hydrochloride | BMS599626 Hydrochloride | BMS 599626 Hydrochloride | AC-480 Hydrochloride | AC 480 Hydrochloride |
| Inhibitors Related | (S)-Afatinib | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Erlotinib hydrochloride | Erlotinib | Neratinib | Afatinib | Chalcone | Genistein | Khellin | Gefitinib |
| Related Compound Libraries | Anti-Colorectal Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Hematonosis Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
