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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $37 | In Stock | |
5 mg | $87 | In Stock | |
10 mg | $133 | In Stock | |
25 mg | $253 | In Stock | |
50 mg | $447 | In Stock | |
100 mg | $659 | In Stock | |
1 mL x 10 mM (in DMSO) | $109 | In Stock |
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. |
Targets&IC50 | HER1:22 nM, HER2:32nM, HER4:190 nM |
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]. |
Alias | AC480 Hydrochloride |
Molecular Weight | 567.01 |
Formula | C27H28ClFN8O3 |
Cas No. | 873837-23-1 |
Smiles | Cl.Cc1c(NC(=O)OC[C@@H]2COCCN2)cn2ncnc(Nc3ccc4n(Cc5cccc(F)c5)ncc4c3)c12 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 90.0 mg/mL (158.7 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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