Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BMS-599626 (AC480) has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.
ターゲット&IC50 | HER1:20 nM, HER2:30 nM, HER4:190 nM |
In vitro | In vivo administration of BMS-599626, ranging from 60 mg/kg to 240 mg/kg, resulted in a dose-dependent inhibition of Sal2 tumor growth, demonstrating effective antitumor activity in its KPL-4 human breast cancer xenografts. The maximum tolerated dose was identified as 180 mg/kg. Similarly, this compound exhibited comparable antitumor activities in other HER2-amplified xenograft models as well as in various HER1-overexpressing xenograft models. |
In vivo | MS-599626 effectively inhibits the proliferation of tumor cells expressing high levels of HER1 and/or HER2, including Sal2, BT474, N87, KPL-4, HCC202, HCC1954, HCC1419, AU565, ZR-75-30, MDA-MB-175, GEO, and PC9 cells, with IC50 values of 0.24 μM, 0.31 μM, 0.45 μM, 0.38 μM, 0.94 μM, 0.34 μM, 0.75 μM, 0.63 μM, 0.51 μM, 0.84 μM, 0.90 μM, and 0.34 μM, respectively. BMS-599626 selectively inhibits the enzymatic activity of recombinant HER1 and HER2 kinases, with IC50 values of 20 nM and 30 nM, respectively. It significantly enhances the radiosensitivity of HN-5 cells expressing EGFR and Her2 by promoting cell cycle redistribution and inhibiting DNA repair. Furthermore, BMS-599626 also inhibits HER4, albeit with lower potency, showing an IC50 of 190 nM. However, it does not significantly inhibit the proliferation of the ovarian tumor cell line A2780 and the fibroblast cell line MRC5, which do not express HER1 or HER2. |
別名 | AC480 |
分子量 | 530.55 |
分子式 | C27H27FN8O3 |
CAS No. | 714971-09-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: <1 mg/mL
DMSO: 104 mg/mL (196 mM)
Ethanol: 16 mg/mL (30.2 mM)
You can also refer to dose conversion for different animals. 詳細
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BMS-599626 714971-09-2 Angiogenesis JAK/STAT signaling MAPK Tyrosine Kinase/Adaptors Src HER MEK EGFR antitumor Epidermal growth factor receptor Sal2 inhibit cells ErbB-1 AC-480 proliferation KPL4 AC480 GEO AC 480 Inhibitor HER1 cancer autophosphorylation BMS 599626 selective BMS599626 inhibitor