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- 详细信息
- 文献和实验
- 技术资料
- 英文名:
N-(3-(5-(2-Aminopyrimidin-4-yl)-2-(tert-butyl)thiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide methanesulfonate
- 供应商:
上海安毕达生物科技有限公司
- CAS号:
1195768-06-9
- 规格:
50μL/1mL/1mg/5mg/10mg/25mg/50mg/100mg
| 规格: | 50μL | 产品价格: | ¥129.0 |
|---|---|---|---|
| 规格: | 1mL | 产品价格: | ¥616.0 |
| 规格: | 1mg | 产品价格: | ¥186.0 |
| 规格: | 5mg | 产品价格: | ¥279.0 |
| 规格: | 10mg | 产品价格: | ¥393.0 |
| 规格: | 25mg | 产品价格: | ¥501.0 |
| 规格: | 50mg | 产品价格: | ¥968.0 |
| 规格: | 100mg | 产品价格: | ¥1430.0 |
Dabrafenib (GSK2118436, 1 μM) combined with 0.01 μM GSK1120212 suppresses over 90% of cell growth in NRAS mutant clones and effectively reduces S6P phosphorylation in A375 cells1. Dabrafenib reduces polyphosphate-mediated vascular barrier permeability, decreases inflammatory biomarkers, and inhibits leukocyte adhesion/migration and the activation/production of nuclear factor-κB, tumor necrosis factor-α, and interleukin-62. Dabrafenib also inhibits HMGB1 release and downregulates HMGB1-dependent inflammatory responses, enhancing the expression of cell adhesion molecules in human endothelial cells3.
Dabrafenib (GSK2118436, 1 μM) combined with 0.01 μM GSK1120212 suppresses over 90% of cell growth in NRAS mutant clones and effectively reduces S6P phosphorylation in A375 cells1.
Dabrafenib reduces polyphosphate-mediated vascular barrier permeability, decreases inflammatory biomarkers, and inhibits leukocyte adhesion/migration and the activation/production of nuclear factor-κB, tumor necrosis factor-α, and interleukin-62.
Dabrafenib also inhibits HMGB1 release and downregulates HMGB1-dependent inflammatory responses, enhancing the expression of cell adhesion molecules in human endothelial cells3.
Dabrafenib treatment results in predominantly immature reproductive tracts with no ovulation signs, similar to controls, but with keratinized and histologically open vaginas5.
Dabrafenib treatment results in predominantly immature reproductive tracts with no ovulation signs, similar to controls, but with keratinized and histologically open vaginas5.
溶解方案(细胞实验)
DMSO 中的溶解度 : 20.83 mg/mL (33.83 mM; 超声助溶 (<60°C); 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 (4.06 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 (4.06 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 (4.06 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。"
"方案 四": "请依序添加每种溶剂:5% DMSO 40% PEG300 5% Tween-80 50% SalineSolubility: 2.5 mg/mL (4.06 mM); 悬浊液; 超声助溶"
"方案 五": "请依序添加每种溶剂:5% DMSO 95% (20% SBE-β-CD in Saline)Solubility: ≥ 2.5 mg/mL (4.06 mM); 澄清溶液"
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文献和实验Lee S, et al. Anti-inflammatory effects of dabrafenib on polyphosphate-mediated vascular disruption. Chem Biol Interact. 2016 Jul 22.
Jung B, et al. Anti-septic effects of dabrafenib on HMGB1-mediated inflammatory responses. BMB Rep. 2016 Apr;49(4):214-9.
Posobiec LM, et al. Early Vaginal Opening in Juvenile Female Rats Given BRAF-Inhibitor Dabrafenib Is Not Associated with Early Physiologic Sexual Maturation. Birth Defects Res B Dev Reprod Toxicol. 2015 Dec;104(6):244-52.
Detection of BCR-ABL Mutations and Resistance to Imatinib Mesylate
The major mechanism of imatinib resistance for patients with chronic myeloid leukemia (CML) is clonal expansion of leukemic cells with mutations in the Bcr-Abl fusion tyrosine kinase that reduce the capacity of imatinib to inhibit kinase
-4 and C-5 centers ( 3 ). After formatron of the mesylate, from the recycled material the amine function is introduced through azrde displacement of the mesylate, followed by reduction ( 4 ) and protectron with the t -BOC group. Finally, the lactone
Inhibitors of Cellular Signaling Targets: Designs and Limitations
. Because of their central role in cellular signaling, as well as their primary role in disease progression, protein kinases are attractive therapeutic targets (2 ,3 ). Seven molecules targeting protein kinases, imatinib mesylate (Gleevec) and trastuzumab (Herceptin
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