AES-135
|
|
|
- CAS号:
- 2361659-61-0
- 英文名:
- Benzamide, 4-[[[4-(1,1-dimethylethyl)phenyl]methyl][2-[[(4-fluorophenyl)sulfonyl][(2,3,4,5,6-pentafluorophenyl)methyl]amino]acetyl]amino]-N-hydroxy-
- 英文别名:
- AES135,HDAC,HDAC3,HDAC11,pancreatic,HDAC6,anti-tumor,Inhibitor,AES 135,Histone deacetylases,inhibit,AES-135;Benzamide, 4-[[[4-(1,1-dimethylethyl)phenyl]methyl][2-[[(4-fluorophenyl)sulfonyl][(2,3,4,5,6-pentafluorophenyl)methyl]amino]acetyl]amino]-N-hydroxy-
- 中文名:
- AES-135
- 中文别名:
- 化合物AES-135
- CBNumber:
- CB85563085
- 分子式:
- C33H29F6N3O5S
- 分子量:
- 693.66
- MOL File:
- 2361659-61-0.mol
|
|
|
AES-135化学性质
-
储存条件:
-
Store at -20°C
-
|
-
溶解度:
-
DMSO : 100 mg/mL (144.16 mM; Need ultrasonic)
-
|
-
形态:
-
Solid
-
|
-
颜色:
-
White to off-white
-
|
AES-135性质、用途与生产工艺
AES-135 是一种基于羟肟酸的 HDAC 抑制剂，可延长胰腺癌原位小鼠模型的存活时间。AES-135 抑制 HDAC3、HDAC6、HDAC8 和 HDAC11，IC50 范围为190-1100 nM。
|
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.
|
AES-135
上下游产品信息
上游原料
下游产品
2361659-61-0, AES-135 相关搜索:
- 标准品
- C33H29F6N3O5S
- 化合物AES-135
- 2361659-61-0
- AES135,HDAC,HDAC3,HDAC11,pancreatic,HDAC6,anti-tumor,Inhibitor,AES 135,Histone deacetylases,inhibit,AES-135
- Benzamide, 4-[[[4-(1,1-dimethylethyl)phenyl]methyl][2-[[(4-fluorophenyl)sulfonyl][(2,3,4,5,6-pentafluorophenyl)methyl]amino]acetyl]amino]-N-hydroxy-