Gemcitabine HCl
(Synonyms: 盐酸吉西他滨; LY 188011 hydrochloride) 目录号 : GC14447
Gemcitabine HCl是化学合成的脱氧胞苷衍生物，是一种DNA合成抑制剂，可在体外抑制人血清对氧磷酶1（PON1）活性，IC50值为26.610mM。此外，Gemcitabine HCl还可用于癌症的治疗，如乳腺癌、膀胱癌和胰腺癌等。
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.
Gemcitabine HCl是化学合成的脱氧胞苷衍生物，是一种DNA合成抑制剂，可在体外抑制人血清对氧磷酶1（PON1）活性，IC50值为26.610mM。此外，Gemcitabine HCl还可用于癌症的治疗，如乳腺癌、膀胱癌和胰腺癌等[1-3]。
Gemcitabine HCl可抑制多种细胞活性，IC50值为240.4±29.0μM（CCRF-CEM/dCK−/−细胞）、14.7±2.8nM（TC-1细胞）、36.7 ± 5.1μM（TC-1-GR细胞）、49.7 ± 17.7nM（MIA PaCa-2细胞）、2.12±0.11（MCF-7细胞）和2.40±0.15μM（MDA-MB-231细胞）[2-3]。在胰腺癌细胞系COLO 357和L3.6pl中，Gemcitabine HCl可以显著抑制细胞生长并促进细胞凋亡[4]。
在胰腺癌患者来源的异种移植小鼠模型中，Gemcitabine HCl（100mg/kg）处理的小鼠肿瘤中LPAR4表达显着升高[5]。在原位植入COLO 357细胞的SCID小鼠中，Gemcitabine HCl（80mg/kg）可抑制小鼠肿瘤生长，可使肿瘤重量减少27%[4]。Gemcitabine HCl（5mg/kg）可抑制裸鼠异种移植模型中肿瘤的生长，并且hsa-miR-3178下调增加了体内肿瘤细胞对Gemcitabine HCl的敏感性[6]。
| 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 | |
| 别名 | 盐酸吉西他滨; LY 188011 hydrochloride | ||
| 化学名 | 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 | ||
| 分子式 | C9H11F2N3O4.HCI | 分子量 | 299.66 |
| 溶解度 | ≥ 7.49mg/mL in Water; 25 mg/mL in DMSO (ultrasonic and warming and heat to 60°C) | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
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Quality Control & SDS
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- Purity: >99.50%
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