Borussertib

¥2,800.00

规格: 5mg

CAS 号:Borussertib
英文名字:1800070-77-2
质量标准:>98%,BR
SKU: MB0368-1 分类: , 标签:

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

Akt (Cell-free assay)
0.8 nM

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

  • Cell lines:Breast, bladder, pancreas, and endometrium cancer cell lines harboring genetic alterations in the PI3K/AKT and RAS/MAPK pathways
  • Concentrations:30 µM to 0.1 nM
  • Incubation Time:96 h
  • Method:

— (Only for Reference)

动物实验

Animal Models:RjOrl:SWISS mice (aged 8-10 weeks)
Formulation:PBS/PEG200 (60:40) for oral and intraperitoneal administration; dissolved in DMSO for intravenous injection
Dosages:20 mg/kg (Oral/IP); 2 mg/kg (IV)
Administration:by oral gavage/intraperitoneal/IV
(Only for Reference)

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

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规格

5mg

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