2409479-29-2
2409479-29-2 結(jié)構(gòu)式
基本信息
1-Propanone, 1-[4-[(1R)-1-[2-[[6-[6-(dimethylamino)-4-pyrimidinyl]-1H-benzimidazol-2-yl]amino]-4-pyridinyl]ethyl]-1-piperazinyl]-3,3,3-trifluoro-
物理化學(xué)性質(zhì)
常見問題列表
| 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%. |