购物车
- 全部删除
- 您的购物车当前为空
JR-AB2-011 是一种选择性 mTORC2抑制剂,IC50值为 0.36 μM。JR-AB2-011 通过阻断 Rictor-mTOR 联合体 (Ki: 0.19 μM) 抑制 mTORC2 活性,并且具有抗多形性胶质母细胞瘤 (GBM) 的活性。
为众多的药物研发团队赋能,
让新药发现更简单!
JR-AB2-011 是一种选择性 mTORC2抑制剂,IC50值为 0.36 μM。JR-AB2-011 通过阻断 Rictor-mTOR 联合体 (Ki: 0.19 μM) 抑制 mTORC2 活性,并且具有抗多形性胶质母细胞瘤 (GBM) 的活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 666 | 现货 | |
5 mg | ¥ 1,630 | 现货 | |
10 mg | ¥ 2,630 | 现货 | |
25 mg | ¥ 4,470 | 现货 | |
50 mg | ¥ 6,370 | 现货 | |
100 mg | ¥ 8,730 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,790 | 现货 |
产品描述 | JR-AB2-011 is a selective mTORC2 inhibitor with an IC 50 value of 0.36 μM. JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association ( K i : 0.19 μM) and is cytotoxic in glioblastoma [1]. |
靶点活性 | mTORC2:0.36 μM |
体外活性 | JR-AB2-011 (1 μM; 24 hours) shows good anti-GBM properties, blocks mTORC2 signaling and Rictor association with mTOR [1]. JR-AB2-011 (0.5-2 μM; 48 hours) displays the least toxicity to normal neurons with no significant cytotoxic effects for concentrations up to 10 mM compared to CID613034 [1]. Apoptosis Analysis [1] Cell Line: U87 GBM cells; LN229 GBM cells Concentration: 1 μM Incubation Time: 24 hours Result: Had good anti-GBM properties and blocked mTORC2 signaling and Rictor association with mTOR. Cell Cytotoxicity Assay [1] Cell Line: Normal mature human neurons Concentration: 0.5, 1, 2 μM Incubation Time: 48 hours Result: Displayed the least toxicity to normal neurons with no significant cytotoxic effects for concentrations up to 10 mM. |
体内活性 | Mice receiving JR-AB2-011 (4 mg/kg; daily i.p. for 10 days; 20 mg/kg; daily i.p. for 10 days) at either dosing regimen show significant inhibition of tumor growth rate (JR-AB2-011 at 4 mg/kg/d; 74% inhibition at end of dosing period; tumor growth delay 10.0 days; JR-AB2-011 at 20 mg/kg/d; 80% inhibition at end of dosing period; tumor growth delay 12.0 days) as compared to mice receiving vehicle alone [1]. Animal Model: LN229 cells in female C.B.-17-scid (Taconic) mice [1] Dosage: 4 mg/kg; 20 mg/kg Administration: Daily i.p.; 10 days Result: Either dosing regimen displayed marked inhibition of tumor growth rate as compared to mice receiving vehicle alone. |
分子量 | 398.28 |
分子式 | C17H14Cl2FN3OS |
CAS No. | 2411853-34-2 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 61.5 mg/mL (154.41 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
|
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.