Borussertib
分子式：C36H32N6O3分子量： 596.68
简介：Borussertib是AKT的共价变构抑制剂，对野生型AKT的IC50值为0.8 nM，Ki值为2.2 nM。
物理性状及指标：
外观：……………………粉末
溶解性：…………………DMSO: 100 mg/mL (167.59 mM)
含量：……………………>98%
储存温度：-20℃，避光防潮密闭干燥
生物活性
|
描述 |
Borussertib是AKT的共价变构抑制剂，对野生型AKT的IC50值为0.8 nM，Ki值为2.2 nM。 | ||
|
靶点 |
|
||
|
体外 |
Borussertib exhibits excellent cellular activity in the nanomolar range. The EC50 values (cell viability assay) of borussertib in AN3CA, T47D, ZR-75-1, MCF-7, BT-474 and KU-19-19 cells are 191 nM, 48 nM, 5 nM, 277 nM, 373 nM and 7770 nM, respectively. Borussertib specifically binds to two non-catalytic cysteines in AKT at positions 296 and 310 by decorating allosteric ligands with electrophilic warheads at suitable positions, thus enabling the irreversible stabilization of the inactive conformation. Borussertib potently inhibits proliferation of PI3K/PTEN-mutated cell lines. | ||
|
体内 |
Borussertib reveals a good pharmacokinetic profile with reasonable microsomal stability in human and murine microsomes. PK studies are carried out in mice (2 mg/kg intravenous; 20 mg/kg oral gavage; 20 mg/kg, intraperitoneal), Despite a rather low oral bioavailability (<5%), reaching only a maximum plasma concentration of 78 ng/mL (0.13 µM), There is a significantly higher bioavailability upon intraperitoneal administration (39.6%), with maximum plasma levels of 683 ng/mL (1.14 µM). | ||
|
细胞实验 |
— (Only for Reference) |
||
|
动物实验 |
Animal Models:RjOrl:SWISS mice (aged 8-10 weeks) |
储液配置及储存：按表中溶解性配置；如溶解困难，可以通过快速搅拌，超声或温和加热（在45-60°C下水浴）。液体稳定性报道的很少，建议现配现用，如需储存，建议：-20℃1-3月；-80℃ 3-6月。
| 浓度/体积/质量 |
1 mg |
5 mg |
10 mg |
| 1 mM | 1.6759 mL | 8.3797 mL | 16.7594 mL |
| 5 mM | 0.3352 mL | 1.6759 mL | 3.3519 mL |
| 10 mM | 0.1676 mL | 0.8380 mL | 1.6759 mL |
| 50 mM | 0.0335 mL | 0.1676 mL | 0.3352 mL |
●我司产品为非无菌包装，若用于细胞培养，请提前做预处理，除去热原细菌，否则会导致染菌。
●部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，以上数据仅供参考交流研究之用。
我司所售出产品仅供于科研研究用途（非临床科研研究），每次销售产品行为都适用于我司网上所列明的通用销售条款。