Gemcitabine HCl |
| Catalog No.GC14447 |
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.
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.
| Cell experiment [1]: | |
Cell lines | FPAC-1, SW1990, SUIT-2, MIA PaCa-2 and PANC-1 cells |
Preparation Method | Pancreatic cancer cells were treated with Gemcitabine HCl. After 24 hours, cell viability was measured using the Cell Counting Kit-8. |
Reaction Conditions | 0.01,0.1,1,10 and 100μM, 24h |
Applications | Gemcitabine HCl inhibited the viability of CFPAC-1, SW1990, SUIT-2, MIA PaCa-2 and PANC-1 cells. MIA PaCa-2 and PANC-1 cells showed higher resistance to Gemcitabine HCl compared to other cell lines. |
| Animal experiment [2]: | |
Animal models | Pancreatic cancer patient-derived xenograft mouse model |
Preparation Method | 1–2mm3 PDX fragments (n=8 patient tumor samples) were implanted to pancreas of NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice. Tumor growth was monitored by weekly ultrasound imaging. Once a tumor size reached 50–100mm3, the mouse was recruited randomly and subsequently treated with vehicle or 100mg/kg Gemcitabine HCl (intraperitoneal injection) twice a week for up to 6 weeks. |
Dosage form | 100mg/kg, Twice a week, 6 weeks, i.p. |
Applications | After 6 weeks of treatment, LPAR4 expression was significantly higher in tumors from Gemcitabine HCl-treated mice compared to the control group. |
References: [1] Zhang W, Fan Y, Zhang J, Shi D, Yuan J, Ashrafizadeh M, Li W, Hu M, Abd El-Aty AM, Hacimuftuoglu A, Linnebacher M, Cheng Y, Li W, Fang S, Gong P, Zhang X. Cell membrane-camouflaged bufalin targets NOD2 and overcomes multidrug resistance in pancreatic cancer. Drug Resist Updat. 2023 Nov;71:101005. [2] 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. | |
| Cas No. | 122111-03-9 | SDF | |
| Chemical Name | 4-amino-1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one;hydrochloride | ||
| Canonical SMILES | C1=CN(C(=O)N=C1N)[C@H]2C([C@@H]([C@H](O2)CO)O)(F)F | ||
| Formula | C9H11F2N3O4.HCI | M.Wt | 299.66 |
| Solubility | ≥ 7.49mg/mL in Water; 25 mg/mL in DMSO (ultrasonic and warming and heat to 60°C) | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3371 mL | 16.6856 mL | 33.3712 mL |
| 5 mM | 0.6674 mL | 3.3371 mL | 6.6742 mL |
| 10 mM | 0.3337 mL | 1.6686 mL | 3.3371 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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