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/ Gemcitabine

吉西他滨 /Gemcitabine {[allProObj[0].p_purity_real_show]}

货号：A433642 同义名： LY 188011;DDFC

Gemcitabine（LY 188011）是一种嘧啶核苷类似物抗代谢物和抗肿瘤剂，阻碍DNA合成和修复，导致自噬和凋亡。

Gemcitabine 化学结构 CAS号：95058-81-4
Gemcitabine 化学结构
CAS号：95058-81-4
Gemcitabine 3D分子结构
CAS号：95058-81-4
Gemcitabine 化学结构 CAS号：95058-81-4
Gemcitabine 3D分子结构 CAS号：95058-81-4
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Gemcitabine 纯度/质量文件 产品仅供科研

货号：A433642 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]
• Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]
• ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]
• ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]
• Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]
更多 >
产品名称 DNA synthesis ↓ helicase ↓ RdRp ↓ ribonucleotide reductase ↓ tRNA synthetase ↓ YB-1 ↓ 其他靶点 纯度
Fexinidazole ✔ 98%
Daptomycin ✔ 98%
Blasticidin S·HCl ✔ 98%
Metronidazole ✔ 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

 		98%
Triglycidyl isocyanurate ✔ p53 98+%
Nedaplatin ✔ 99%+
Bendamustine ✔ 98+%
Trifluridine ✔ 98%
Robinetin ✔ 99%+
Carboplatin ✔ 99%
Cidofovir ✔ 99%
Cisplatin ✔ 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

 		98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

 		99%+
Oxaliplatin ✔ 98%
YK-4-279 ✔ 99%+
ML216 +

BLM636-1298, IC50: 0.97 μM

BLMfull-length, IC50: 2.98 μM

 		99%+
RK-33 ✔ 98%
Brr2-IN-3 ✔ 99%+
Phen-DC3 Trifluoromethanesulfonate ✔ 98%
Favipiravir ✔ 99%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

 		99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

 		97%
Didox ✔ 98%
(E)-3-AP ✔ 99%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

 		99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, IC50: 46.11 nM

Leucyl-tRNA synthetase, Kd: 42.1 nM

 		98%
SU056 +

YB-1, IC50: 1.73 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 Autophagy ↓ 其他靶点 纯度
SBI-0206965 +++

ULK1, IC50: 108 nM

ULK2, IC50: 711 nM

 		97%
Hydroxychloroquine sulfate ✔ 99%
Valproic acid sodium ✔ HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

 		99%+
MRT68921 hydrochloride ++++

ULK1, IC50: 2.9 nM

ULK2, IC50: 1.1 nM

 		99%+
ROC-325 ✔ 99%+
Autophinib +++

Autophagy, IC50: 40 nM

 		99%
Lys05 ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Gemcitabine 生物活性

描述 Gemcitabine (dFdCTP, LY-188011, NSC 613327, (+)-2'-Deoxy-2',2'-difluorocytidine) is a deoxycytidine analogue that has a spectrum of activity against solid tumors[1]. Gemcitabine can inhibit DNA synthesis through a combination of two actions. The first, gemcitabine can inhibit ribonucleotide reductase (RR) and then cause the decrease of the deoxynucleotide pool sizes for DNA repair and synthesis[2]. The second, gemcitabine inhibit DNA synthesis through competition with dCTP and incorporation into DNA[3]. Gemcitabine can induce S-phase arrest and cell growth inhibition[4].
作用机制 Gemcitabine, as nucleoside analogue, can inhibit DNA synthesis through inhibition of ribonucleotide reductase and incorporation into DNA[5].

Gemcitabine 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
23132-87 Growth Inhibition Assay IC50=43.05 nM SANGER
647-V Growth Inhibition Assay IC50=0.248 nM SANGER
697 Growth Inhibition Assay IC50=6.25 nM SANGER
769-P Growth Inhibition Assay IC50=0.123 nM SANGER

Gemcitabine 动物研究

Dose Mice (i.p.): min = 3.5 mg/kg, max = 240 mg/kg[6]
Administration i.p.
Pharmacokinetics
Animal Rats[7]
Dose 5 mg/kg
Administration i.v.
Cmax 8078 ± 4176 μg/l
AUC0→∞ 25288 ± 11487 μg/l·h
Vz 1.788 ± 1.265 l/kg
AUC0→t 23480 ± 13061 μg/l·h
CL 0.255 ± 0.161 l/h/kg
t1/2z 5.04 ± 2.06 h

Gemcitabine 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02240238 Solid Tumors Phase 1 Phase 2 Recruiting November 30, 2019 United States, California ... 展开 >> California Cancer Associates for Research and Excellence Recruiting Encinitas, California, United States, 92024 UC San Diego Moores Cancer Center Recruiting La Jolla, California, United States, 92037 Pacific Hematology Oncology Associates Recruiting San Francisco, California, United States, 94115 United States, Illinois Northwestern University Feinberg School of Medicine Recruiting Chicago, Illinois, United States, 60611 United States, Massachusetts Tufts Medical Center Recruiting Boston, Massachusetts, United States, 02111 United States, North Carolina University of North Carolina at Chapel Hill Recruiting Chapel Hill, North Carolina, United States, 27599 United States, Ohio University Hospitals Case Medical Center Recruiting Cleveland, Ohio, United States, 44121 United States, Oklahoma University of Oklahoma Health Sciences Center Recruiting Oklahoma City, Oklahoma, United States, 73104 United States, Texas University of Texas Southwestern Medical Center Recruiting Dallas, Texas, United States, 75390 MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Bulgaria Multiprofile Hospital for Active Treatment Serdika EOOD Recruiting Sofia, Sofia-Grad, Bulgaria, 1632 Complex Oncology Center - Shumen EOOD Recruiting Shumen, Bulgaria, 9700 Italy Istituto Scientifico Romagnolo Per Lo Studio E La Cura Dei Tumori IRST Recruiting Meldola, Italy, 47014 ASST Grande Ospedale Metropolitano Niguarda - Presidio Ospedaliero Ospedale Niguarda Ca' Granda Recruiting Milano, Italy, 20162 Poland Wojewodzki Szpital Specjalistyczny im. Ludwika Rydygiera w Krakowie Recruiting Krakow, Poland, 31826 Med-Polonia Sp. z o.o. Recruiting Poznan, Poland, 60693 Romania Fundeni Clinical Institute Recruiting Bucharest, Romania, 22328 Coltea Clinical Hospital Recruiting Bucharest, Romania, 30171 Prof Dr I Chiricuta Institute of Oncology Recruiting Cluj-Napoca, Romania, 400015 Oncology Center Sfantul Nectarie Recruiting Craiova, Romania, 200347 Euroclinic Oncology Center SRL Recruiting Iasi, Romania, 700106 Institutul Regional de Oncologie Iasi Recruiting Iasi, Romania, 700483 收起 <<
NCT00610740 - Completed - -
NCT00610740 Cervical Cancer ... 展开 >> Endometrial Cancer Ovarian Cancer 收起 << Phase 2 Completed - United States, Minnesota ... 展开 >> University of Minnesota Cancer Center Minneapolis, Minnesota, United States, 55455 收起 <<

Gemcitabine 参考文献

[1]Hertel LW, Boder GB, et al. Evaluation of the antitumor activity of gemcitabine (2',2'-difluoro-2'-deoxycytidine). Cancer Res. 1990 Jul 15;50(14):4417-22.

[2]Heinemann V, Xu YZ, et al. Cellular elimination of 2',2'-difluorodeoxycytidine 5'-triphosphate: a mechanism of self-potentiation. Cancer Res. 1992 Feb 1;52(3):533-9.

[3]Huang P, Chubb S, et al. Action of 2',2'-difluorodeoxycytidine on DNA synthesis. Cancer Res. 1991 Nov 15;51(22):6110-7.

[4]Shi Z, Azuma A, et al. S-Phase arrest by nucleoside analogues and abrogation of survival without cell cycle progression by 7-hydroxystaurosporine. Cancer Res. 2001 Feb 1;61(3):1065-72.

[5]Action of 2',2'-Difluorodeoxycytidine on DNA Synthesis

[6]Boven E, Schipper H, et al. The influence of the schedule and the dose of gemcitabine on the anti-tumour efficacy in experimental human cancer. Br J Cancer. 1993 Jul;68(1):52-6.

[7]Chu W, Tian P, et al. Improving Plasma Stability and Bioavailability In Vivo of Gemcitabine Via Nanoparticles of mPEG-PLG-GEM Complexed with Calcium Phosphate. Pharm Res. 2018 Oct 11;35(12):230.

Gemcitabine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.80mL

0.76mL

0.38mL

19.00mL

3.80mL

1.90mL

37.99mL

7.60mL

3.80mL

Gemcitabine 技术信息

CAS号95058-81-4
分子式C9H11F2N3O4
分子量 263.2
别名 LY 188011;DDFC;NSC 613327
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Sealed in dry,Store in freezer, under -20°C
溶解度

DMSO: 250 mg/mL(949.85 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 6 mg/mL(22.8 mM)，配合低频超声，并水浴加热至45℃助溶

无水乙醇: 12 mg/mL(45.59 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方

PO 0.5% CMC-Na 30 mg/mL suspension

Tags: Gemcitabine | LY 188011;DDFC;NSC 613327 | Nucleoside Antimetabolite/Analog | Autophagy | DNA/RNA Synthesis | AmBeed-信号通路专用抑制剂 | Gemcitabine 纯度/质量文件 | Gemcitabine 亚型比较 | Gemcitabine 生物活性 | Gemcitabine 细胞研究 | Gemcitabine 动物研究 | Gemcitabine 临床数据 | Gemcitabine 参考文献 | Gemcitabine 实验方案 | Gemcitabine 技术信息

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