规格 | 价格 | 库存 | 数量 |
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2mg |
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5mg |
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10mg |
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25mg |
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Other Sizes |
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体外研究 (In Vitro) |
体外活性:在体外,CEP-1347 在临床相关浓度下有效诱导分化,并抑制来自胶质母细胞瘤以及胰腺癌和卵巢癌的人类癌症干细胞的自我更新和肿瘤启动能力,且不损害其活力。正常成纤维细胞和神经干细胞。激酶测定:CEP-1347(也称为 KT7515)是在 Narcodiopsis 细菌肉汤中发现的天然产物 K-252a 的衍生物,是一种新型有效的 JNK 抑制剂,对 JNK1 的 IC50 为 30 nM。细胞测定:卵巢中过度表达的生存素的敲低癌症干细胞(CSC)的化疗耐药性导致对紫杉醇的敏感性增加。 CEP-1347(一种已知对人类安全性的混合谱系激酶抑制剂)在临床相关浓度下进行治疗,可降低卵巢 CSC 中生存素的表达,并使它们对紫杉醇敏感。
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体内研究 (In Vivo) |
在体内,CEP-1347 的 10 天全身给药剂量低于小鼠当量(相当于人类 2 年安全给药剂量的 1/10),足以有效减少已建立肿瘤内的肿瘤起始癌症干细胞在小鼠中。此外,相同的治疗方案显着延长了接受神经胶质瘤干细胞原位植入的小鼠的生存期。总之,这些发现表明 CEP-1347 是癌症干细胞靶向治疗的有前途的候选者,并且需要进一步的临床和临床前研究来评估其在癌症治疗中的功效。
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动物实验 |
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参考文献 |
:Anticancer Res.2018 Aug;38(8):4535-4542;Oncotarget.2017 Oct 24;8(55):94872-94882.
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分子式 |
615.76
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分子量 |
C33H33N3O5S2
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CAS号 |
156177-65-0
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相关CAS号 |
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SMILES |
N12C3=C(C4=C1C1=C(C5=C(N1[C@]1([H])O[C@@]2(C)[C@H](C(OOC)=O)C1)C=CC(CSCC)=C5)C1C(=O)NCC=14)C=C(CSCC)C=C3
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化学名 |
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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) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 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。 |
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) 。
CEP-1347induces the differentiation of cancer stem cells into non-cancer stem cells.Oncotarget.2017 Oct 24;8(55):94872-94882. th> |
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CEP-1347treatment deprives cancer stem cells of their sphere forming ability.Cells treated without (Control) or withCEP-1347(300 nM for PANC-1 CSLC, 200 nM for the others) for 6 days were subjected to a sphere formation assay in the absence ofCEP-1347.Oncotarget.2017 Oct 24;8(55):94872-94882. td> |
Systemically administeredCEP-1347selectively targets and inhibits tumor-initiating cancer stem cells within tumors in tumor-bearing mice.Oncotarget.2017 Oct 24;8(55):94872-94882. td> |
CEP-1347inhibits the tumor-initiating capacity of cancer stem cells.Oncotarget.2017 Oct 24;8(55):94872-94882. th> |
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Short-term systemicCEP-1347treatment inhibits tumor formation by glioma stem cells in an orthotopic brain tumor model.Mice implanted intracranially with GS-Y03 cells underwent a daily i.p. injection ofCEP-1347(1.5 mg/kg/day) for 10 days.Oncotarget.2017 Oct 24;8(55):94872-94882. td> |