Gemcitabine

製品コードS1714 バッチS171404

印刷

化学情報

 Chemical Structure Synonyms LY-188011, NSC 613327 Storage
(From the date of receipt)
powder, 4°C,3 years (in the dark) ; in solvent,-80°C,1 year (in the dark)
化学式

C9H11F2N3O4

分子量 263.2 CAS No. 95058-81-4
Solubility (25°C)* 体外 DMSO 52 mg/mL (197.56 mM)
Water 13 mg/mL (49.39 mM)
Ethanol Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/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.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Gemcitabineは、nucleic acid synthesis阻害剤であり、非常に強力で特異的なデオキシシチジンアナログで、化学療法として使用されます。Gemcitabineは強力なp53依存性apoptosisを誘導します。
in vitro

Gemcitabine results in 50% inhibition of growth in the CCRF-CEM human leukemia cell culture assay with IC50 of 1 ng/ml. This compound combined with deoxycytidine provides about a 1000-fold decrease in biological activity.

This chemical combined with C225 results in additive cytotoxic effects that increased with increasing gemcitabine concentrations in human pancreatic carcinoma L3.6pl cells.

It combined with Cisplatin results in synergistic effect in wild-type A2780 and cisplatin-resistant ADDP cells.

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. This compound treatment alone reduces median tumor volume from 538 to 152 mm3. It reduces the production of vascular endothelial growth factor and interleukin 8 in gemcitabine-treated tumors.

This chemical 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.

It 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. This compound combined with Curcumin is also highly effective in suppressing angiogenesis as indicated by a decrease in CD31(+) microvessel density.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 PC cells
濃度 1 μM
反応時間 72 h
実験の流れ

Cells were treated with different concentrations of gemcitabine.

動物実験 動物モデル Female BALB/c nude mice 
投薬量 5 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/2364394/
  • https://pubmed.ncbi.nlm.nih.gov/10815919/
  • https://pubmed.ncbi.nlm.nih.gov/7481849/
  • https://pubmed.ncbi.nlm.nih.gov/16166452/
  • https://pubmed.ncbi.nlm.nih.gov/17440100/
  • https://pubmed.ncbi.nlm.nih.gov/35538494/

カスタマーフィードバック

Data from [Mol Cancer, 2017, 16(1):22]

Data from [Proc Natl Acad Sci USA, 2015, 112(6): 1839-44]

Data from [Nucleic Acids Res, 2014, 42(10), 6436-47]

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人間や獣医の診断であるか治療的な使用のためにでない。

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