规格 | 价格 | 库存 | 数量 |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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体外研究 (In Vitro) |
JK184 旨在通过剂量依赖性抑制神经胶质瘤 (Gli) 依赖性转录活性来抵消 Hh 信号传导。孵育三天后,JK184 显着抑制 HUVEC 增殖,IC50 为 6.3 μg/mL。将指定浓度的化合物给予 Panc-1 和 BxPC-3 细胞后,测量 JK184 的半数抑制浓度 (IC50)(Anc-1 中为 23.7 ng/mL,BxPC-3 中为 34.3 ng/mL)[1 ]。该测定用于评估 JK184 的抗肿瘤作用。与 MCF10a、MTSV1-7、HMLE-shGFP 和 HMLE-pBP 细胞相比,claudin-low 细胞系对 JK184 处理更敏感。在这些细胞系中,JK184 导致 GLI1(神经胶质瘤相关癌基因同源物 1)转录物和蛋白质水平呈剂量依赖性降低。当用 IC50 剂量的 JK184 处理时,用膜联蛋白-V 染色但碘化丙啶 (PI) 检测呈阴性的 HMLE-shEcad 细胞百分比(P<0.0001,t 检验)增加[2]。
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体内研究 (In Vivo) |
JK184(5 mg/kg,静脉注射)是一种有希望的候选抗肿瘤药物,以 Hh 信号为靶点,因为它在皮下 Panc-1 和 BxPC-3 肿瘤模型中显示出良好的抗增殖活性。然而,JK184 的生物利用度和药代动力学特征较低 [1]。
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动物实验 |
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参考文献 |
[1]. Zhang N, et al. Biodegradable polymeric micelles encapsulated JK184 suppress tumor growth through inhibiting Hedgehog signaling pathway. Nanoscale. 2015 Feb 14;7(6):2609-24.
[2]. Colavito SA, et al. Significance of glioma-associated oncogene homolog 1 (GLI1) expression in claudin-low breast cancer and crosstalk with the nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) pathway. Breast Cancer Res. 2014 Sep 25;16 |
分子式 |
C19H18N4OS
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分子量 |
350.44
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CAS号 |
315703-52-7
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相关CAS号 |
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SMILES |
CC1=C(C2=CSC(NC3=CC=C(OCC)C=C3)=N2)N4C=CC=CC4=N1
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别名 |
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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)
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溶解度 (体外) |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.13 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 25.0 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: ≥ 2.5 mg/mL (7.13 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 25.0 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: ≥ 2.5 mg/mL (7.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 | 2.8536 mL | 14.2678 mL | 28.5356 mL | |
5 mM | 0.5707 mL | 2.8536 mL | 5.7071 mL | |
10 mM | 0.2854 mL | 1.4268 mL | 2.8536 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) 。
JK184 is more effective at inhibiting EMT cell proliferation.Breast Cancer Res.2014 Sep 25;16(5):444. th> |
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JK184 inhibits growth of claudin-low cell lines.Breast Cancer Res.2014 Sep 25;16(5):444. td> |
Decrease inGLI1expression inhibits cell migration and anchorage-independent growth.Breast Cancer Res.2014 Sep 25;16(5):444. td> |
EMT and claudin-low cells are insensitive to Hedgehog (Hh) pathway inhibitors.Breast Cancer Res.2014 Sep 25;16(5):444. th> |
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Crosstalk between NFκB and GLI1 signaling pathways.Breast Cancer Res.2014 Sep 25;16(5):444. td> |
Claudin-low cell lines express higher transcript and protein levels ofGLI1.Breast Cancer Res.2014 Sep 25;16(5):444. td> |