Kobe0065
作者：齐岳
发布时间：2023-08-30
09:02:47
点击数：
产品名称：Kobe0065
产品描述：
| 产品描述 | Kobe0065 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; shows potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM. |
| 靶点活性 | c-Raf-1 RBD:46 ± 13 μM(ki) |
| 体外活性 | Kobe0065-family compounds bind to Ras?GTP and exhibit antiproliferative activity toward cancer cells carrying the activated ras oncogenes. The compounds efficiently inhibit the interaction of Ras?GTP with their multiple effectors including Raf, PI3K, and RalGDS and a regulator/effector Sos and show rather broad binding specificity toward various Ras family small GTPases, which may account for their higher potency at the cellular level compared with that of the in vitro binding inhibition[1]. |
| 体内活性 | Kobe0065 has antitumor activity. The compound-treated tumors show a prominent increase of apoptotic cells without any significant body weight loss[1]. |
| 激酶实验 | Determination of lipase activity: For determination of lipase activity, lysates are incubated with a substrate containing radiolabeled [9,10-3H(N)]-triolein. Subsequently, FA are extracted and quantitated by liquid scintilation counting. Data are presented as mean S.D. of triplicate determinations and representative for at least three independent experiments. |
| 细胞实验 | NIH 3T3 cells are transfected with pEF-BOS-HA-H-Ras(G12V) or an empty vector and treated with the 2 and 20 μM compound or the vehicle (DMSO) in the presence of 2% FBS for 1 h. Cell lysate is subjected to detection of c-Raf-1 coimmunoprecipitated with an anti-H-Ras antibody and total c-Raf-1 by Western blotting with an anti-c-Raf-1 antibody. Immunoprecipitated H-Ras(G12V) are detected by an anti-HA antibody.(Only for Reference) |
| 分子量 | 449.79 |
| 分子式 | C15H11ClF3N5O4S |
| CAS No. | 436133-68-5 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: 4.5 mg/mL (10 mM)),with gentle warming
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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