Gemcitabine

カタログ番号 T0251 CAS 95058-81-4

別名: NSC 613327, LY188011

Gemcitabine (LY188011) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.

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Gemcitabine, CAS 95058-81-4

パッケージサイズ	在庫状況	単価(税別)
サンプルについてお問い合わせ
50 mg	在庫あり	￥ 8,000
100 mg	在庫あり	￥ 11,500
200 mg	在庫あり	￥ 13,500
500 mg	在庫あり	￥ 19,500
1 g	在庫あり	￥ 22,500
1 mL * 10 mM (in DMSO)	在庫あり	￥ 11,500

バルクのお問い合わせ

バッチを選択

純度: 100%

COA DATASHEET SDS HPLC HNMR

純度: 100%

COA DATASHEET SDS

純度: 99.67%

COA DATASHEET SDS HNMR HPLC

純度: 99.62%

COA DATASHEET SDS HNMR HPLC

純度: 99%

COA DATASHEET SDS HNMR

COA DATASHEET SDS

バッチの詳細情報はお問い合わせください

生物学的特性に関する説明

化学的特性

保存条件 & 溶解度情報

説明	Gemcitabine (LY188011) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.
ターゲット＆IC50	BxPC-3 cells:18nM, Capan-2 cells:12 nM, MIAPaCa2:40nM
In vitro	METHODS: PDAC-derived paired primary cancer cells (PCCs) PCC-1, PCC-2, PCC-5, PCC-6, and PDAC cells BxPC-3, Mia PaCa-2, and Panc-1 were treated with Gemcitabine (0.001-1000 µM) for 48 h, and the cells were assayed for cell growth inhibition using MTT. RESULTS: Gemcitabine dose-dependently inhibited the growth of PCC-1, PCC-2, PCC-5, PCC-6, BxPC-3, Mia PaCa-2, and Panc-1 cells with IC50 of 1.2/0.3/1.2/4.3/4.2/7.9/10.5 µM, respectively.[1] METHODS: Human pancreatic cancer cells PK-1 were treated with Gemcitabine (30 nM) for 24-48 h. The cell cycle was examined by Flow Cytometry. RESULTS: Gemcitabine induced an increase in the percentage of PK-1 cells in the G0/G1 phase and a decrease in the percentage of S-phase and G2/M cells, and Gemcitabine induced S-phase cell cycle arrest in PK-1 cells. [2] METHODS: Human lung cancer cells SPC-A1 and A549 were transfected with GFP-labeled LC3, incubated with Gemcitabine (5 μM) for 24 h, and then LC3 expression was detected by confocal laser scanning microscopy. RESULTS: The accumulation of LC3-II is a marker of autophagy. Gemcitabine significantly increased the GFP-LC3 spots in the tumor cells, indicating an increase in the level of autophagy. [3]
In vivo	METHODS: To detect anti-tumor activity in vivo, Gemcitabine (20 mg/kg) was intraperitoneally injected into BALB/cAJcl-nu/nu mice bearing human high-grade meningioma tumor HKBMM twice a week for four weeks. RESULTS: Gemcitabine treatment not only inhibited tumorigenesis but also tumor growth. Gemcitabine blocked the cell cycle progression and promoted apoptosis in tumor cells in vivo. Gemcitabine exerted potent anti-tumor activity against high-grade meningiomas through cytostatic and cytotoxic mechanisms. [4] METHODS: To assay antitumor activity in vivo, Gemcitabine (50 mg/kg/twice weekly/peritoneal injection) and DMAPT (40 mg/kg/day/gavage) were administered to LSL-KrasG12D/+; LSL-Trp53R172H; and Pdx-1-Cre mutant mice bearing pancreatic cancer tumors. RESULTS: Gemcitabine or the DMAPT/Gemcitabine combination significantly increased median survival (254.5 or 255 versus 217.5 days) and decreased the incidence and diversity of pancreatic adenocarcinomas. Gemcitabine treatment increased plasma levels of IL-1α, IL-1β, and IL-17 in mice. While DMAPT/Gemcitabine decreased the levels of IL-12p40, MCP-1, MIP-1β, eotaxin and TNF-α, all target genes of κB. [5]
細胞研究	The cytotoxic effect of gemcitabine was evaluated with the MTT assay. SPC-A1 or A549 cells were treated with gemcitabine (0.05–500 lM) for 24 h. Then, 10 ll of MTT (5 mg/ml in PBS) was added to each well and incubated for 4 h at 37 C. Then, the formazan crystals were solubilized with 200 ll DMSO. The absorbance at 570 nm was measured using an automatic multiwell spectrophotometer. The experiment was repeated four times for each group [3].
動物実験	At 1 month of age, LSL-Kras G12D/+; LSL-Trp53 R172H; Pdx-1-Cre mice are randomized into treatment groups (placebo, DMAPT, Gemcitabine, DMAPT/Gemcitabine). Placebo (vehicle=hydroxylpropyl methylcellulose, 0.2% Tween 80 [HPMT]) and DMAPT (40 mg/kg body weight in HPMT) are administered by oral gastric lavage once daily. Gemcitabine (50 mg/kg body weight in PBS) is administered by intraperitoneal injection twice weekly. Mouse weight is monitored weekly. Treatment is continued until mice show signs of lethargy, abdominal distension or weight loss at which time they are sacrificed. Successful excision-recombination events are confirmed in the pancreata of mice by detecting the presence of a single LoxP site [5].

別名	NSC 613327, LY188011
分子量	263.2
分子式	C9H11F2N3O4
CAS No.	95058-81-4

保存条件

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 15 mg/mL (56.99 mM)

5% DMSO+95% Saline: 0.75 mg/mL (2.85 mM)

参考文献

1. Amrutkar M, et al. Differential Gemcitabine Sensitivity in Primary Human Pancreatic Cancer Cells and Paired Stellate Cells Is Driven by Heterogenous Drug Uptake and Processing. Cancers (Basel). 2020 Dec 3;12(12):3628. 2. Namima D, et al. The Effect of Gemcitabine on Cell Cycle Arrest and microRNA Signatures in Pancreatic Cancer Cells. In Vivo. 2020 Nov-Dec;34(6):3195-3203. 3. Wu HM, et al. Gemcitabine-Induced Autophagy Protects Human Lung Cancer Cells from Apoptotic Death. Lung. 2016 Dec;194(6):959-966. 4. Takeda H, et al. Antitumor activity of gemcitabine against high-grade meningioma in vitro and in vivo. Oncotarget. 2017 Jun 29;8(53):90996-91008. 5. Yip-Schneider MT, et al. Dimethylaminoparthenolide and gemcitabine: a survival study using a genetically engineered mouse model of pancreatic cancer. BMC Cancer. 2013 Apr 17;13:194. 6. Lou M, et al. Physical interaction between human ribonucleotide reductase large subunit and thioredoxin increases colorectal cancer malignancy. J Biol Chem. 2017 Jun 2;292(22):9136-9149. 7. Wang Y, et al. Licoricidin enhances gemcitabine-induced cytotoxicity in osteosarcoma cells by suppressing the Akt and NF-κB signal pathways. Chem Biol Interact. 2018 May 18;290:44-51. 8. Thieulent C, Hue E, Sutton G, et al. Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination[J]. Antiviral Research. 2020: 104931 9. Chang Z, Zhang Y, Liu J, et al. GATA1 Promotes Gemcitabine Resistance in Pancreatic Cancer through Antiapoptotic Pathway[J]. Journal of Oncology. 2019 Apr 10;2019:9474273. 10. Liu L, Liu S, Deng P, et al. Targeting the IRAK1-S100A9 Axis Overcomes Resistance to Paclitaxel in Nasopharyngeal Carcinoma[J]. Cancer Research.

引用文献

1. Li Y, Tang S, Shi X, et al.Metabolic classification suggests the GLUT1/ALDOB/G6PD axis as a therapeutic target in chemotherapy-resistant pancreatic cancer.Cell Reports Medicine.2023 2. Shi Y H, Xu Q C, Zhu Y Q, et al. Imatinib facilitates gemcitabine sensitivity by targeting epigenetically activated PDGFC signaling in pancreatic cancer. Molecular Therapy. 2022 3. Zhao F, Huang Y, Zhang Y, et al. SQLE inhibition suppresses the development of pancreatic ductal adenocarcinoma and enhances its sensitivity to chemotherapeutic agents in vitro. Molecular Biology Reports. 2022: 1-9 4. Liu L, Liu S, Deng P, et al. Targeting the IRAK1–S100A9 Axis Overcomes Resistance to Paclitaxel in Nasopharyngeal Carcinoma. Cancer Research. 2021, 81(5): 1413-1425. 5. Sun Y, Ren D, Zhou Y, et al. Histone acetyltransferase 1 promotes gemcitabine resistance by regulating the PVT1/EZH2 complex in pancreatic cancer. Cell Death & Disease. 2021, 12(10): 1-13. 6. Chang Z, Zhang Y, Liu J, et al. GATA1 Promotes Gemcitabine Resistance in Pancreatic Cancer through Antiapoptotic Pathway. Journal of Oncology. 2019 Apr 10;2019:9474273 7. Thieulent C, Hue E, Sutton G, et al. Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination. Antiviral Research. 2020: 104931 8. Xu H, Tan M, Hou G Q, et al.Blockade of DDR1/PYK2/ERK signaling suggesting SH2 superbinder as a novel autophagy inhibitor for pancreatic cancer.Cell Death & Disease.2023, 14(12): 811. 9. Tan X D, Luo C F, Liang S Y.Antihyperlipidemic drug rosuvastatin suppressed tumor progression and potentiated chemosensitivity by downregulating CCNA2 in lung adenocarcinoma.Journal of Chemotherapy.2024: 1-13.

投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください

投与量

mg/kg

動物の平均体重

動物あたりの投与量

動物数

溶媒の組成を入力してください

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

計算するリセット

計算結果:

作業濃度: mg/ml;

DMSO溶液の作成方法: mg あらかじめ溶解した薬剤 μL DMSO (マスター溶液の濃度 mg/mL)，濃度がそのバッチの薬剤のDMSO溶解度を超える場合は、まずご連絡ください。

生体内薬剤の調合法：取る μL DMSO マスター溶液、次に追加 μL PEG300，確実に混ぜてから加える μL Tween 80，確実に混ぜてから加える μL ddH₂O, 確実に混ぜる

お問合せ内容:

必ず順番通りに溶媒を加えてください。ボルテックスミキサーや超音波、湯煎することで溶解しやすくなります

計算器

モル濃度計算機

希釈計算機

再構成計算

分子量計算機

質量

濃度

体積

分子量

モル度計算機では以下の計算が可能です

既知の体積と濃度の溶液を調製するために必要な化合物の質量
質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度

参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか？
［分子量（MW）］の欄に［197.13］と入力してください
[濃度]ボックスに10と入力し、正しい単位（millimolar）を選択します
[容量]ボックスに10と入力し、正しい単位（milliliter）を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

濃度 (開始)

体積 (開始)

濃度 (終了)

体積 (終了)

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2＆V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか？
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度（開始）ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度（終了）ボックスに50を入力し正しい単位(millimolar)を選択してください
体積（終了）ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積（開始）ボックスに表示されます。

分子式

分子量 g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント：化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量（分子量）を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量（分子量）とは、物質の1分子の質量であり、統一された原子質量単位（u）で表されます。(1uは炭素12の1原子の質量の1/12に等しい）
モル質量（molar weight）とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Gemcitabine 95058-81-4 Apoptosis Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair Nucleoside Antimetabolite/Analog DNA/RNA Synthesis inhibit NSC-613327 LY 188011 Inhibitor NSC613327 NSC 613327 LY-188011 LY188011 inhibitor

本ウェブサイトに掲載されている製品は全て研究用試薬です。研究目的以外の用途にはご使用できません。

Gemcitabine

保存条件

溶解度情報

参考文献

引用文献

関連化合物ライブラリー

関連製品

投与量変換

In vivo投与量計算 (透明溶液)

計算器

モル度計算機では以下の計算が可能です

溶液を作るのに必要な希釈率の計算

バイアルを再構成するのに必要な溶媒の量を計算する.

化合物の化学式を入力して、そのモル質量や元素組成を計算します

技術サポート

Keywords