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- 详细信息
- 文献和实验
- 技术资料
- 英文名:
(2E,6E)-2,6-Bis(pyridin-4-ylmethylene)cyclohexanone
- 供应商:
上海安毕达生物科技有限公司
- CAS号:
871361-88-5
- 规格:
50μL/1mL/5mg/10mg/25mg/50mg
| 规格: | 50μL | 产品价格: | ¥119.0 |
|---|---|---|---|
| 规格: | 1mL | 产品价格: | ¥522.0 |
| 规格: | 5mg | 产品价格: | ¥346.0 |
| 规格: | 10mg | 产品价格: | ¥485.0 |
| 规格: | 25mg | 产品价格: | ¥875.0 |
| 规格: | 50mg | 产品价格: | ¥1260.0 |
The PI3K/AKT/mTOR signaling pathway is involved in various cellular processes such as cell proliferation, migration, survival and angiogenesis. The phosphatidylinositol-3,4,5-triphosphate (PIP3) binding function of pleckstrin homology (PH) domain is essential for the activation of oncogenic Akt/PKB kinase3. SC66 is an allosteric Akt inhibitor that affects AKT/mTOR signaling by a decrease in AKT phosphorylation levels and in total protein levels4. After treatment with increasing concentrations of SC-66, activating PIK3CA (E545K, E542K) and inactivating PTEN (R233*) mutations were identified in human cervical cancer. SC-66 effectively inhibited AKT, mTOR and mTOR substrates in C33A cells. SC-66 inhibited glucose uptake via reduced delivery of Glut1 and Glut4 to the cell membrane. SC-66 (1 µg/ml-56%) treatment decreased cell viability through a non-apoptotic mechanism. Decreases in cell viability were enhanced when AKT inhibitors were combined with 2-DG. The scratch assay showed a substantial reduction in cell migration upon SC-66 treatment5. A mouse xenograft tumor model of Hep3B cells was used to demonstrate the effectiveness in vivo of SC66 on HCC. Treatment with 25 mg/Kg SC66 via i.p. injection twice a week significantly reduced tumor volume to 37%. SC66 inhibit HCC cell viability with IC50 values of approximately 0.85 and 0.75 μg/ml at 48 and 72 hours, respectively for HepG2, HA22T/VGH and PLC/PRF/5 cells4.
溶解方案(细胞实验)
DMSO 中的溶解度 : 25 mg/mL (90.47 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)
溶解方案(动物实验)
"方案 一": "请依序添加每种溶剂:10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: ≥ 2.5 mg/mL (9.05 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。"
"方案 二": "请依序添加每种溶剂:10% DMSO 90% (20% SBE-β-CD in Saline)Solubility: ≥ 2.5 mg/mL (9.05 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。"
"方案 三": "请依序添加每种溶剂:10% DMSO 90% Corn OilSolubility: ≥ 2.5 mg/mL (9.05 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。"
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文献和实验Jo H, Lo PK, et al. Deactivation of Akt by a small molecule inhibitor targeting pleckstrin homology domain and facilitating Akt ubiquitination. Proc Natl Acad Sci U S A. 2011 Apr 19;108(16):6486-91.
Jo H, Lo PK, Li Y, Loison F, Green S, Wang J, Silberstein LE, Ye K, Chen H, Luo HR. Deactivation of Akt by a small molecule inhibitor targeting pleckstrin homology domain and facilitating Akt ubiquitination. Proc Natl Acad Sci U S A. 2011 Apr 19;108(16):6486-91.
Cusimano A, Puleio R, D'Alessandro N, Loria GR, McCubrey JA, Montalto G, Cervello M. Cytotoxic activity of the novel small molecule AKT inhibitor SC66 in hepatocellular carcinoma cells. Oncotarget. 2015 Jan 30;6(3):1707-22.
Rashmi R, DeSelm C, Helms C, Bowcock A, Rogers BE, Rader JL, Grigsby PW, Schwarz JK. AKT inhibitors promote cell death in cervical cancer through disruption of mTOR signaling and glucose uptake. PLoS One. 2014 Apr 4;9(4):e92948.
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