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Gemcitabine

Catalog No. T0251 CAS 95058-81-4

Synonyms: 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

Pack Size	Availability	Price/USD
50 mg	In stock	$ 34.00
100 mg	In stock	$ 50.00
200 mg	In stock	$ 58.00
500 mg	In stock	$ 85.00
1 g	In stock	$ 98.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 100%

Purity: 99.67%

Purity: 99.62%

Purity: 99%

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Description	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.
Targets&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]
Cell Research	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].
Animal Research	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].

Synonyms	NSC 613327, LY188011
Molecular Weight	263.2
Formula	C9H11F2N3O4
CAS No.	95058-81-4

Storage

store at low temperature,keep away from direct sunlight

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

Solubility Information

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

DMSO: 15 mg/mL (56.99 mM)

References and Literature

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.

Citations

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Pediatric Drug Library Fluorochemical Library FDA-Approved & Pharmacopeia Drug Library DNA Damage & Repair Compound Library

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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

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