BMS-599626 Hydrochloride
作者：齊岳
發布時間：2023-08-25
08:58:44
點擊數：
產品名稱：BMS-599626 Hydrochloride
產品描述：
| 產品描述 | BMS-599626 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. BMS-599626 Hydrochloride inhibits human epidermal growth factor receptors (HER) HER1, HER2 and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors. |
| 靶點活性 | HER1:22 nM, HER2:32nM, HER4:190 nM |
| 體外活性 | 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]. |
| 體內活性 | BMS-599626 Hydrochloride given before and during irradiation improved the radioresponse of HN5 tumors in vivo [2]. |
| 別名 | AC480 Hydrochloride |
| 分子量 | 567.01 |
| 分子式 | C27H28ClFN8O3 |
| CAS No. | 873837-23-1 |
存儲
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 90.0 mg/mL (158.7 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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