Gemcitabine HCl |
| رقم الكتالوجGC14447 |
Gemcitabine Hydrochloride (LY 188011 Hydrochloride) هو مضاد للميتابوليت النظير للبيريميدين وعامل مضاد للأورام. يمنع Gemcitabine Hydrochloride تخليق وإصلاح الحمض النووي ، مما يؤدي إلى الالتهام الذاتي والاستماتة.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 122111-03-9
Sample solution is provided at 25 µL, 10mM.
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Gemcitabine HCl is a chemically synthesized deoxycytidine derivative and a DNA synthesis inhibitor that can inhibit human serum Paraoxonase 1（PON1） activity in vitro with an IC50 value of 26.610mM. In addition, Gemcitabine HCl can also be used to treat cancers such as breast cancer, bladder cancer and pancreatic cancer [1-3].
Gemcitabine HCl can inhibit a variety of cell activities, with IC50 values of 240.4±29.0μM (CCRF-CEM/dCK−/− cells), 14.7±2.8nM (TC-1 cells), and 36.7 ± 5.1μM (TC-1-GR cells), 49.7 ± 17.7nM (MIA PaCa-2 cells), 2.12 ± 0.11 (MCF-7 cells) and 2.40 ± 0.15μM (MDA-MB-231 cells)[2-3]. In pancreatic cancer cell lines COLO 357 and L3.6pl, Gemcitabine HCl can significantly inhibit cell growth and increase apoptosis[4].
In a pancreatic cancer patient-derived xenograft mouse model, LPAR4 expression was significantly increased in tumors of mice treated with Gemcitabine HCl (100mg/kg) [5]. In SCID mice orthotopically implanted with COLO 357 cells, Gemcitabine HCl (80mg/kg) inhibited tumor growth in mice and reduced tumor weight by 27%[4]. Gemcitabine HCl (5mg/kg) can inhibit tumor growth in xenotransplantation models in nude mice, and down-regulation of hsa-miR-3178 increases the sensitivity of tumor cells to Gemcitabine HCl[6].
References:
[1] Türkeş C, Söyüt H, Beydemir Ş. Inhibition effects of gemcitabine hydrochloride, acyclovir, and 5-fluorouracil on human serum paraoxonase-1 (hPON1): in vitro[J]. Open J Biochem, 2013, 1: 10-15.
[2] Yalcin T E, Ilbasmis-Tamer S, Takka S. Antitumor activity of gemcitabine hydrochloride loaded lipid polymer hybrid nanoparticles (LPHNs): In vitro and in vivo[J]. International journal of pharmaceutics, 2020, 580: 119246.
[3] Lansakara, P.D., B.L. Rodriguez, and Z. Cui, Synthesis and in vitro evaluation of novel lipophilic monophosphorylated gemcitabine derivatives and their nanoparticles. Int J Pharm, 2012. 429(1-2): p. 123-34.
[4] Banerjee, S., et al., Molecular evidence for increased antitumor activity of gemcitabine by genistein in vitro and in vivo using an orthotopic model of pancreatic cancer. Cancer Res, 2005. 65(19): p. 9064-72.
[5] Wu C, Rakhshandehroo T, Wettersten HI, Campos A, von Schalscha T, Jain S, Yu Z, Tan J, Mose E, Childers BG, Lowy AM, Weis SM, Cheresh DA. Pancreatic cancer cells upregulate LPAR4 in response to isolation stress to promote an ECM-enriched niche and support tumour initiation. Nat Cell Biol. 2023 Feb;25(2):309-322.
[6] Gu J, Huang W, Wang X, Zhang J, Tao T, Zheng Y, Liu S, Yang J, Chen ZS, Cai CY, Li J, Wang H, Fan Y. Hsa-miR-3178/RhoB/PI3K/Akt, a novel signaling pathway regulates ABC transporters to reverse gemcitabine resistance in pancreatic cancer. Mol Cancer. 2022 May 10;21(1):112.
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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