Gemcitabine

Catalog No.S1714

Gemcitabine is a very potent and specific deoxycytidine analogue, used as chemotherapy.

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Gemcitabine  Chemical Structure

Gemcitabine Chemical Structure
Molecular Weight: 263.2

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Gemcitabine is available in the following compound libraries:

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Product Description

Biological Activity

Description Gemcitabine is a very potent and specific deoxycytidine analogue, used as chemotherapy.
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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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... Click to View More Cell Line Experimental Data

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]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Hertel LW, et al. Cancer Res, 1990, 50(14), 4417-4422.

[2] Bruns CJ, et al. Clin Cancer Res, 2000, 6(5), 1936-1948.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02538432 Not yet recruiting Prostate Cancer|Non-Small Cell Lung Cancer|Breast Cancer University of Maryland January 2017 Phase 2
NCT02767557 Not yet recruiting Unresectable Pancreatic Carcinoma Herlev Hospital|Celgene|Roche Pharma AG October 2016 Phase 2
NCT02806687 Not yet recruiting Pancreatic Adenocarcinoma University Hospital, Toulouse|BIOTHERAPY department of th  ...more University Hospital, Toulouse|BIOTHERAPY department of the clinical center of investigation- CIC 1436, Toulouse|InvivoGen Therapeutics October 2016 Phase 2
NCT02741388 Not yet recruiting B-cell Lymphoma The Lymphoma Academic Research Organisation|Karyopharm Th  ...more The Lymphoma Academic Research Organisation|Karyopharm Therapeutics, Inc September 2016 Phase 1
NCT02723838 Not yet recruiting Muscle-invasive Transitional Cell Carcinoma of the Bladder Oncolytics Biotech September 2016 Phase 1

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Chemical Information

Download Gemcitabine SDF
Molecular Weight (MW) 263.2
Formula

C9H11F2N3O4

CAS No. 95058-81-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms LY-188011, NSC 613327
Solubility (25°C) * In vitro DMSO 15 mg/mL (56.99 mM)
Water 16 mg/mL warming (60.79 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo water 16mg/mL
* <1 mg/ml means slightly soluble or 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 Name 2'-​deoxy-​2',​2'-​difluoro-cytidine

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.

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.

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

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

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