Gemcitabine HCl
(Synonyms: 盐酸吉西他滨; LY 188011 hydrochloride) 目录号 : GC14447
An anticancer nucleoside analog
Cas No.:122111-03-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment: [1] | |
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Cell lines |
COLO 357 and L3.6pl cells |
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Preparation method |
The solubility of this compound in DMSO is |
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Reacting condition |
25 nM, 72 hours |
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Applications |
Cells were either pretreated with genistein (25 μmol/L) alone or in combination with a single dose of gemcitabine (25 nmol/L), and viable cells were evaluated at 96 hours posttreatment by MTT assay. Treatment with either genistein or gemcitabine alone for 96 hours resulted in only 25% to 30% loss of viability of COLO 357 and L3.6pl cells. However, pretreatment with genistein for 24 hours followed by treatment with gemcitabine resulted in the loss of 60% to 80% of viable cells in both the cell types investigated. These results suggests that the combination of genistein with low therapeutic doses of gemcitabine elicits significantly greater inhibition of cancer cell growth compared with either agent, suggesting that lower toxic side effects are likely to occur in normal cells. |
| Animal experiment: [1] | |
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Animal models |
Female nude mice (ICR-SCID) injected with COLO 357 or L3.6pl cells |
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Dosage form |
Intravenous injection, 80 mg/kg body weight, every other day for a total of three injections |
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Application |
Mice were randomized into the following treatment groups (n = 7): (a) untreated control; (b) only gemcitabine; (c) genistein, 1 mg genistein/d/mouse, everyday orally for 10 days; and (d) genistein and gemcitabine. Single modality treatment with either genistein or gemcitabine alone in mice harboring COLO 357 cells caused 13% and 27% reduction in tumor weight, respectively, compared with control tumors. Under identical experimental conditions, combination of genistein and gemcitabine treatment showed significant decrease in tumor weight compared with untreated control, genistein alone–, or gemcitabine alone– treated group. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Banerjee S, Zhang Y, Ali S, et al. Molecular evidence for increased antitumor activity of gemcitabine by genistein in vitro and in vivo using an orthotopic model of pancreatic cancer. Cancer research, 2005, 65(19): 9064-9072. |
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Gemcitabine HCl is an inhibitor of DNA synthesis with the IC50 value of 240.4±29.0 μM (CCRF-CEM/dCK−/− cells), 14.7±2.8 nM (TC-1 cells), 36.7 ± 5.1 μM (TC-1-GR cells), and 50 nM (PANC1 cells) [1].
DNA synthesis is the natural or artificial creation of DNA molecules and can be defined as DNA replication, polymerase chain reaction, and gene synthesis. It is reported that DNA synthesis process plays an important role in a variety of cancers, many drugs have been made to target this process to inhibit tumor growth or metastasis [2] [3].
Gemcitabine HCl is a DNA synthesis inhibitor. When tested with pancreatic cancer cell line COLO 357 and L3.6pl, Gemcitabine HCl treatment following genistein which sensitized cells to Gemcitabine HCL significantly inhibited cell growth and increased cell apoptosis [4]. In MIA PaCa-2 cells, Gemcitabine HCl showed markedly cytotoxicity to cells with the IC50 value of 49.7 ± 17.7 nM via inhibiting the activity of dDNA [1].
In SCID mice bearing COLO 357 cells orthotopically implanted, compared with control group, treated both genistein and gemcitabine significantly decreased (75%, P < 0.01) tumor growth and body weight [4].
References:
[1].Lansakara, P.D., B.L. Rodriguez, and Z. Cui, Synthesis and in vitro evaluation of novel lipophilic monophosphorylated gemcitabine derivatives and their nanoparticles. Int J Pharm, 2012. 429(1-2): p. 123-34.
[2].Kostyrev, O.A. and T.A. Leont'eva, [Autoradiographic study of DNA systhesis in muscle and connective tissue cells of the heart during exposure to isopropylnorepinephrine]. Biull Eksp Biol Med, 1973. 76(7): p. 108-11.
[3].Mathews, L.A., et al., Increased expression of DNA repair genes in invasive human pancreatic cancer cells. Pancreas, 2011. 40(5): p. 730-9.
[4].Banerjee, S., et al., Molecular evidence for increased antitumor activity of gemcitabine by genistein in vitro and in vivo using an orthotopic model of pancreatic cancer. Cancer Res, 2005. 65(19): p. 9064-72.
| Cas No. | 122111-03-9 | SDF | |
| 别名 | 盐酸吉西他滨; LY 188011 hydrochloride | ||
| 化学名 | 4-amino-1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one;hydrochloride | ||
| Canonical SMILES | C1=CN(C(=O)N=C1N)[C@H]2C([C@@H]([C@H](O2)CO)O)(F)F | ||
| 分子式 | C9H11F2N3O4.HCI | 分子量 | 299.66 |
| 溶解度 | ≥ 7.49mg/mL in Water; 25 mg/mL in DMSO (ultrasonic and warming and heat to 60°C) | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Abstract
An UV spectrophotometry-based method accurately, reliably and rapidly determines GMCT with low cost and simple procedures.
Abstract
As an antitumor agent, Gemcitabine HCL, which induces apoptosis through caspase activation, exhibited lower cytotoxicity in CCRF-CEM-AraC-8C, CCRF-CEM/dCK(-/-) and TC-1-GR cell lines but higher cytotoxicity in wild type CCRF-CEM cell lines than GemC18-NPs.
Abstract
Daily oral administration of LY2334737 of 6 mg/kg for 21 days is equivalent to weekly i.v. administration of gemcitabine HCL of 240 mg/kg for 3 weeks in mice bearing a patient mesothelioma tumor PXF 1118 or a non-small cell lung cancer tumor LXFE 927.
Abstract
Gemcitabine HCL is an approved antitumor agent that has lower cytotoxicity than monophosphorylated gemcitabine derivatives in dCK deficient cells and cells with overexpressing RRM1 or RRM2.