AES-135
| 中文名称 | AES-135 |
|---|---|
| 中文同义词 | 化合物AES-135;化合物AES-135,10 MM DMSO 溶液 |
| 英文名称 | Benzamide, 4-[[[4-(1,1-dimethylethyl)phenyl]methyl][2-[[(4-fluorophenyl)sulfonyl][(2,3,4,5,6-pentafluorophenyl)methyl]amino]acetyl]amino]-N-hydroxy- |
| 英文同义词 | Benzamide, 4-[[[4-(1,1-dimethylethyl)phenyl]methyl][2-[[(4-fluorophenyl)sulfonyl][(2,3,4,5,6-pentafluorophenyl)methyl]amino]acetyl]amino]-N-hydroxy-;AES135,HDAC,HDAC3,HDAC11,pancreatic,HDAC6,anti-tumor,Inhibitor,AES 135,Histone deacetylases,inhibit,AES-135;AES-135, 10 mM in DMSO |
| CAS号 | 2361659-61-0 |
| 分子式 | C33H29F6N3O5S |
| 分子量 | 693.66 |
| EINECS号 | |
| 相关类别 | 标准品 |
| Mol文件 | 2361659-61-0.mol |
| 结构式 |  |
AES-135 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | DMSO：100 mg/mL（144.16 mM；需要超声波） |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
|
HDAC6 190 nM (IC 50 ) |
HDAC11 636 nM (IC 50 ) |
HDAC3 654 nM (IC 50 ) |
HDAC8 1100 nM (IC 50 ) |
AES-135 inhibits cancer cells growth with IC 50 values of 2.3 µM, 1.4 µM, 0.27 µM, 0.94 µM, 1.9 µM, 2.72 µM, 2.1 µM, 15.0 µM, 1.6 µM and 19.2 µM for BT143, BT189, D425, D458, MV4-11, MOLM-13, MDA-MB-231, K562, PC-3 and MRC-9 cells, respectively.
AES-135 (50 mg/kg; intraperitoneal injection; 5 days a week; for 1 month) treatment significantly increases survival of C57Bl/6 mice implanted with KPC2 cells.
NSG mice are dosed with a single 20 mg/kg intraperitoneal (IP) injection, and blood is taken at 0.5 h, 1 h, 2 h, 4 h, 8 h, and 24 h. AES-135 achieved μM concentrations in the blood, reaching C
max
7452 ng/mL (10.74 μM) within 30 min, which is sustained for 8 h. The blood concentration of AES-135 is dose dependent, achieving an average of 323 ng/mL (0.47 μM) with 10 mg/kg dosing and 1829 ng/mL (2.64 μM) with 40 mg/kg. AES-135 shows an impressive pharmacokinetic profile in mice with an in vivo half-life of 5.0 h.
| Animal Model: | C57Bl/6 mice injected with KPC2 cells |
| Dosage: | 50 mg/kg |
| Administration: | Intraperitoneal injection; 5 days a week; for 1 month |
| Result: | Significantly increased survival of mice. |