Gemcitabine (LY-188011)

For research use only.

Catalog No.S1714 Synonyms: NSC 613327

157 publications

Gemcitabine (LY-188011) Chemical Structure

CAS No. 95058-81-4

Gemcitabine (LY-188011, NSC 613327), a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.

Selleck's Gemcitabine (LY-188011) has been cited by 157 publications

Purity & Quality Control

Choose Selective DNA/RNA Synthesis Inhibitors

Biological Activity

Description Gemcitabine (LY-188011, NSC 613327), a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.
In vitro

Gemcitabine results in 50% inhibition of growth in the CCRF-CEM human leukemia cell culture assay with IC50 of 1 ng/ml. Gemcitabine combined with deoxycytidine provides about a 1000-fold decrease in biological activity. [1] Gemcitabine combined with C225 results in additive cytotoxic effects that increased with increasing gemcitabine concentrations in human pancreatic carcinoma L3.6pl cells. [2] Gemcitabine combined with Cisplatin results in synergistic effect in wild-type A2780 and cisplatin-resistant ADDP cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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H460 NULheppQSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MmDoRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKNE[wJINmdGy|IHjhdoJwemmwZzDkc41qdmGwdDDu[YdifGm4ZTDwOVMh[2:wc4TyeYN1NCCJSUWwJF0hOC5yMEKwPFUh|ryPLh?= NHPKW4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUOwNVA5PSd-MkmzNFExQDV:L3G+
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MIAPaCa2 NV3EVWFUS3m2b4TvfIlkcXS7IHHzd4F6 NYrMWnlDPzJiaILz M4PXU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGenbXPpeIFjcW6nLYLld4l{fGGwdDDoeY1idiCPSVHQZWNiOiClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEOuN{DPxE1w NF;0WVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUOyPFY2Pid-MkmzNlg3PTZ:L3G+
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p70S6K1 / p-S6 / HIF-1α ; 

PubMed: 27765914     


Cells were treated with different doses of gemcitabine (0, 1.5 and 2.5 μM), the expression levels of p70S6K1, p-S6 and HIF-1α were determined by Western blotting. GAPDH is used as an internal control.

PARP / Cleaved PARP / Cleaved caspase-3 / phopho-p38 / p38 / p-JNK / JNK / p-c-Jun; 

PubMed: 24409315     


AsPC-1, BxPC-3, and COLO-357 cells were incubated for the indicated times with 100 ng/ml, 10 ng/ml, and 5 ng/ml gemcitabine, respectively, and analyzed by immunoblotting. 

27765914 24409315
Immunofluorescence
Bim1; 

PubMed: 27177084     


Gemcitabine enhanced nuclear accumulation of Bmi1 by immunofluorescence staining. The graphs shown are representative results of three independently repeated experiments. Scale bar, 50 μm.

27177084
Growth inhibition assay
Cell viability; 

PubMed: 27765914     


A and B. Pancreatic adenocarcinoma cells Bxpc-3 (A) and Panc-1 (B) were treated with gemcitabine (GEM) for 48 h at different doses. The cell viability was analyzed by CCK-8 assay, and normalized to cells without gemcitabine treatment. 

27765914
In vivo Gemcitabine combined with C225 results in growth inhibition, tumor regression, and abrogation of metastasis in L3.6pl tumors established in the pancreas of nude mice. Gemcitabine treatment alone reduces median tumor volume from 538 to 152 mm3. Gemcitabine reduces the production of vascular endothelial growth factor and interleukin 8 in gemcitabine-treated tumors. [2] Gemcitabine is able to dramatically and specifically reduces the number of myeloid suppressor cells found in the spleens of animals bearing large tumors with no significant reductions in CD4(+) T cells, CD8(+) T cells, NK cells, macrophages, or B cells. [4] Gemcitabine combined with curcumin shows significant reductions in volume (P = 0.008 versus control; P = 0.036 versus gemcitabine alone), Ki-67 proliferation index (P = 0.030 versus control), NF-kappaB activation, and expression of NF-kappaB-regulated gene products (cyclin D1, c-myc, Bcl-2, Bcl-xL, cellular inhibitor of apoptosis protein-1, cyclooxygenase-2, matrix metalloproteinase, and vascular endothelial growth factor) compared with tumors from control mice treated with olive oil only. Gemcitabine combined with Curcumin is also highly effective in suppressing angiogenesis as indicated by a decrease in CD31(+) microvessel density. [5]

Protocol

Solubility (25°C)

In vitro DMSO 52 mg/mL (197.56 mM)
Water 52 mg/mL warmed (197.56 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 263.2
Formula

C9H11F2N3O4

CAS No. 95058-81-4
Storage powder
in solvent
Synonyms NSC 613327
Smiles C1=CN(C(=O)N=C1N)C2C(C(C(O2)CO)O)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04871321 Recruiting Drug: nab-paclitaxel plus gemcitabine-cisplatin Biliary Tract Cancer|Cholangiocarcinoma|Gallbladder Cancer CHA University|Dong-A Pharmaceutical July 1 2021 --
NCT04983407 Recruiting Drug: AVB-S6-500|Drug: Nab paclitaxel|Drug: Gemcitabine Pancreatic Adenocarcinoma Aravive Inc. July 28 2021 Phase 1|Phase 2
NCT04896320 Not yet recruiting Drug: Tucatinib Breast Cancer Stage IV Providence Health & Services|Seagen Inc. July 2021 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    What is the difference between gemcitabine(S1714 ) and Gemcitabine HCl (S1149)?

  • Answer:

    Gemcitabine HCl is the HCl salt form of Gemcitabine. They have the same biological activities. The free base(S1714) dissolves better in DMSO, and the hydrochloride (S1149) dissolves better in water.

DNA/RNA Synthesis Signaling Pathway Map

Related DNA/RNA Synthesis Products

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID