BAY-985
BAY-985 性质
| 沸点 | 753.3±70.0 °C(Predicted) |
|---|---|
| 密度 | 1.373±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：50 mg/mL（90.32 mM） |
| 形态 | 固体 |
| 酸度系数(pKa) | 10.06±0.10(Predicted) |
BAY-985 用途与合成方法
| Target | Value |
|
TBK1
(in low ATP assay) | 2 nM |
|
IKKε
(Cell-free assay) | 2 nM |
|
TBK1
(in high ATP assay) | 30 nM |
|
pIRF3
(Cell-free assay) | 74 nM |
BAY-985 inhibits FLT3, RSK4, DRAK1, and ULK1 with IC
50
s of 123, 276, 311, and 7930 nM, respectively.
BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 (IRF3) with an IC
50
of 74 nM.
BAY-985 is active in cellular mechanistic assay and shows anti-proliferative activity in a few cancer cell lines with IC
50
s of 900 and 7260 nM for SK-MEL2 (NRAS and TP53 mutated) and ACHN (CDKN2A mutated) cells, respectively.
Cell Proliferation Assay
| Cell Line: | ACHN and SK-MEL-2 cell lines |
| Concentration: | |
| Incubation Time: | 96 hours |
| Result: | Inhibited proliferation in SK-MEL2 and ACHN cells with IC 50 s of 900 and 7260 nM, respectively. |
BAY-985 (200 mg/kg; p.o.; b.i.d.; 111 days) results in weak antitumor efficacy.
BAY-985 shows high clearance (CL
b
= 4.0 L/h/kg, ca. 95% hepatic extraction), large volume of distribution at steady state (V
ss
=2.9 L/kg) and a short terminal half-life (t
1/2
=0.79 h).
| Animal Model: | Female NMRI nude mice bearing SK-MEL-2 human melanoma xenograft model |
| Dosage: | 200 mg/kg |
| Administration: | Applied p.o.; twice daily (b.i.d.) continuously 111 days |
| Result: |
Treatment resulted in weak antitumor efficacy with a T/C
tumor weight
ratio of 0.6.
The treatment was well tolerated, with a maximum body weight loss of less than 10%. |
BAY-985 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-04-30 | HY-133117 | 1 mg | 1714 | ||
| 2024-04-30 | HY-133117 | BAY-985 | 2409479-29-2 | 5mg | 4500 |
