规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mM * 1 mL in DMSO |
|
||
10mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
2g |
|
||
5g |
|
||
Other Sizes |
|
靶点 |
DNA synthesis (Capan2 cells) ( IC50 = 12 nM ); DNA synthesis (BxPC3 cells) ( IC50 = 18 nM ); DNA synthesis (MIAPaCa2 cells) ( IC50 = 40 nM ); DNA synthesis (PANC1 cells) ( IC50 = 50 nM )
|
||
---|---|---|---|
体外研究 (In Vitro) |
体外活性:吉西他滨诱导 BxPC-3、PANC-1 和 MIA PaCa-2 细胞中的 NF-κB 活性,并降低 BxPC-3 和 PANC-1 细胞中 NF-κB 抑制剂 IκBα 的水平。用低剂量吉西他滨处理 BxPC-3 细胞 48 小时会导致 NF-κB 结合呈剂量依赖性增加。相比之下,用较高吉西他滨剂量处理 48 小时的 BxPC-3 细胞中 NF-κB DNA 结合减少;然而,用这些较高剂量进行 24 小时处理会增加 BxPC-3 细胞中 NF-κB 的结合。细胞测定:将 BxPC-3、MIA PaCa-2 和 PANC-1 细胞接种到 96 孔板中。 24小时后,用媒介物、DMAPT和/或吉西他滨再处理细胞24小时或48小时。使用细胞死亡检测 ELISA 来定量细胞凋亡,以检测细胞质组蛋白相关 DNA 片段的量并相对于载体处理的细胞进行表达。
|
||
体内研究 (In Vivo) |
与 PBS 治疗的小鼠相比,吉西他滨治疗的小鼠瘤内 NF-κB 活性显着升高(1.3 至 1.8 倍),表明吉西他滨也诱导 NF-κB 激活。
|
||
细胞实验 |
在 96 孔板中,接种 BxPC-3、MIA PaCa-2 和 PANC-1 细胞。 24小时后用媒介物、DMAPT和/或吉西他滨进一步处理细胞24或48小时。使用细胞死亡检测 ELISA,通过计算细胞质组蛋白相关 DNA 片段的数量来测量与载体处理的细胞相关的细胞凋亡。
|
||
动物实验 |
|
||
参考文献 |
|
分子式 |
C9H11F2N3O4.HCI
|
|
---|---|---|
分子量 |
299.66
|
|
精确质量 |
299.05
|
|
元素分析 |
C, 36.07; H, 4.04; Cl, 11.83; F, 12.68; N, 14.02; O, 21.36
|
|
CAS号 |
122111-03-9
|
|
相关CAS号 |
|
|
外观&性状 |
White solid powder
|
|
SMILES |
C1=CN(C(=O)N=C1N)[C@H]2C([C@@H]([C@H](O2)CO)O)(F)F.Cl
|
|
InChi Key |
OKKDEIYWILRZIA-OSZBKLCCSA-N
|
|
InChi Code |
InChI=1S/C9H11F2N3O4.ClH/c10-9(11)6(16)4(3-15)18-7(9)14-2-1-5(12)13-8(14)17;/h1-2,4,6-7,15-16H,3H2,(H2,12,13,17);1H/t4-,6-,7-;/m1./s1
|
|
化学名 |
4-amino-1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one;hydrochloride
|
|
别名 |
Abbreviations: dFdC; dFdCyd; LY188011; LY-188011; LY 188011; gemcitabine; Gemzar
|
|
HS Tariff Code |
2934.99.9001
|
|
存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
溶解度 (体外) |
|
|||
---|---|---|---|---|
溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: Saline: 20 mg/mL Solubility in Formulation 5: 60 mg/mL (200.23 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3371 mL | 16.6856 mL | 33.3712 mL | |
5 mM | 0.6674 mL | 3.3371 mL | 6.6742 mL | |
10 mM | 0.3337 mL | 1.6686 mL | 3.3371 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02769832 | Active Recruiting |
Drug: Nab-paclitaxel Drug: Gemcitabine |
Small Cell Lung Cancer (SCLC) |
Muhammad Furqan | August 29, 2016 | Phase 2 |
NCT00479128 | Active Recruiting |
Drug: Bortezomib Drug: Gemcitabine |
Solid Tumor Urethral Cancer |
M.D. Anderson Cancer Center | September 28, 2006 | Phase 1 |
NCT03520790 | Active Recruiting |
Drug: Gemcitabine Other: Placebo |
Pancreatic Cancer | Dana-Farber Cancer Institute | December 5, 2018 | Phase 1 Phase 2 |
NCT03558087 | Active Recruiting |
Drug: Nivolumab Drug: Gemcitabine |
Bladder Cancer | Matthew Galsky | July 13, 2018 | Phase 2 |
NCT03507491 | Active Recruiting |
Drug: Gemcitabine Drug: Nab-paclitaxel |
Cancer | Emory University | August 27, 2018 | Phase 1 |
Cytotoxicity of I3C and gemcitabine (GEM) at clinical relevant concentrations in hTERT-HPNE and BxPC-3 cells cells. Anticancer Res . 2011 Oct;31(10):3171-80. td> |
Effect of I3C in combination with gemcitabine (GEM) on hENT1 protein expression in pancreatic cancer cell lines. Anticancer Res . 2011 Oct;31(10):3171-80. td> |
Combined inhibition of hTrx1 and RRM1 produced a synergistic anticancer effect in cancer cells and xenograft mice. A, SW480 or SW620 cells were treated with the indicated concentrations of gemcitabine or PX-12 for 72 h, and cell viability was measured with Cell Counting Kit-8 assays. J Biol Chem . 2017 Jun 2;292(22):9136-9149. td> |