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My CartCAS：95058-81-4
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 95058-81-4 |
| Name | Gemcitabine |
| Molecular Formula | C9H11F2N3O4 |
| Molecular Weight | 263.2 |
| Solubility | Soluble in Water/DMSO ≥3mg/mL |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 619-100-6 |
| MDL | MFCD00869720 |
| SMILES | O=C1N(C=CC(N)=N1)[C@H]2C(F)([C@@H]([C@H](O2)CO)O)F |
| InChIKey | SDUQYLNIPVEERB-QPPQHZFASA-N |
| InChI | InChI=1S/C9H11F2N3O4/c10-9(11)6(16)4(3-15)18-7(9)14-2-1-5(12)13-8(14)17/h1-2,4,6-7,15-16H,3H2,(H2,12,13,17)/t4-,6-,7-/m1/s1 |
| PubChem CID | 60750 |
| Target Point | DNA/RNA Synthesis |
| Passage | Cell Cycle;DNA Damage/DNA Repair |
| Background | Gemcitabine is a DNA synthesis inhibitor. Is a pyrimidine nucleoside analog. It can inhibit DNA synthesis and repair, leading to autophagy and apoptosis. |
| Biological Activity | Gemcitabine (NSC 613327;LY188011) 是一种 DNA合成 抑制剂，抑制 BxPC-3，Mia Paca-2，PANC-1，PL-45 和 AsPC-1细胞生长的 IC50 分别为 37.6, 42.9, 92.7, 89.3 和 131.4 nM[1-5]。 |
| In Vitro | MTS测定证明，15nM的吉西他滨，50μM的吲哚-3-甲醇(I3C)和该组合不影响hTERT-HPNE细胞活力。然而，用15nM的吉西他滨，50μM的I3C和该组合治疗分别导致BxPC-3细胞31％，19％和72％的细胞死亡[1]。 |
| In Vivo | 治疗LSL-KrasG12D/+; LSL-Trp53R172H;与安慰剂组相比，使用吉西他滨(50 mg/kg，ip)或组合DMAPT /吉西他滨的Pdx-1-Cre小鼠显著增加中位生存时间超过30天(254.5 [P = 0.015]或255天[ P = 0.018]分别为217.5天)[2]。吉西他滨可通过大鼠气管内喷雾给药，无明显毒性，最大耐受剂量为4mg/kg，每周一次，持续9周。在剂量为2，4和6 mg/kg时，吉西他滨的毒性低于口服给药[3]。 |
| Cell Experiment | 将细胞(人胰腺细胞系，Mia PaCa-2，BxPC-3，AsPC-1，PANC-1，PL-45和正常胰腺导管上皮细胞，hTERT-HPNE细胞)接种到96孔板中(3000细胞/孔)一式三份。孵育过夜后，更换培养基并用I3C和/或NBMPR处理细胞24小时。再次更换培养基，并在存在或不存在相同浓度的I3C和/或NBMPR的情况下，在含有不同浓度的吉西他滨的培养基中培养细胞48小时。然后按照制造商的说明对细胞进行CellTiter 96 AQueous One Solution Cell Proliferation Assay(MTS)。在加入20μLMTS试剂/孔后2小时测量490nm处的吸光度[1]。 |
| Animal Experiment | 小鼠[2]在1个月大时，LSL-KrasG12D/+; LSL-Trp53R172H;将Pdx-1-Cre小鼠随机分入治疗组(安慰剂，DMAPT，吉西他滨，DMAPT /吉西他滨)。安慰剂(载体=羟丙基甲基纤维素，0.2％吐温80 [HPMT])和DMAPT(HPMT中40mg/kg体重)通过每天一次口服洗胃施用。每周两次通过腹膜内注射施用吉西他滨(PBS中50mg/kg体重)。每周监测小鼠体重。继续治疗直至小鼠出现嗜睡，腹胀或体重减轻的迹象，此时将其处死。通过检测单个LoxP位点的存在，在小鼠胰腺中确认成功的切除 - 重组事件。大鼠[3]该研究在80只雌性Wistar大鼠中进行，初始重量约为250g。通过耳标识别动物并如下分组。将40只大鼠分成5组，每组8只：4组通过气管内喷雾分别以2，4，6和8mg/kg的剂量肺组织给予吉西他滨(LD2，LD4，LD6，LD8组)和一组接受0.9％盐水载体溶液(组LDv)的喷雾给药。将剩余的40只大鼠分成5组，每组8只：4组分别通过管饲法分别以2，4，6和8mg/kg的剂量口服递送吉西他滨(OD2，OD4，OD6，OD8组)，组通过管饲法接受相同体积的0.9％盐水(组ODv)。该协议包括以1周为间隔的九个会话。在两个疗程之间，将动物保持在标准实验室条件下，并在每个笼子中由四只动物的一组饲养，其中有垫料并且可以自由获得颗粒食物和自来水。将笼子放置在与抽吸系统连接的封闭腔室中。 |
| Data Literature Source | [1]. Wang H，et al. Enhanced efficacy of Gemcitabine by indole-3-carbinol in pancreatic cell lines: the role of human equilibrativenucleoside transporter 1. Anticancer Res. 2011 Oct;31(10):3171-80. [2]. Yip-Schneider MT，et al. Dimethylaminoparthenolide and Gemcitabine: a survival study using a genetically engineered mouse model of pancreatic cancer. BMC Cancer. 2013 Apr 17;13:194. [3]. Gagnadoux F，et al. Safety of pulmonary administration of gemcitabine in rats. J Aerosol Med. 2005 Summer;18(2):198-206 [4]. Lou M，et al. Physical interaction between human ribonucleotide reductase large subunit and thioredoxin increases colorectal cancer malignancy. J Biol Chem. 2017 Jun 2;292(22):9136-9149. [5]. Wang Y，et al. Licoricidin enhances gemcitabine-induced cytotoxicity in osteosarcoma cells by suppressing the Akt and NF-κB signal pathways. Chem Biol Interact. 2018 May 18;290:44-51. |
| Unit | Bottle |
| Specification | 10mg 10mM*1mL in DMSO 50mg |
是一种 DNA合成 抑制剂。是一种嘧啶核苷类似物。可以抑制 DNA 合成 (DNA synthesis) 和修复，导致细胞自噬 (autophagy) 和凋亡 (apoptosis)。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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Pan Y, et al. Microsyst Nanoeng. 2020 Mar 9;6:23.
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