Gemcitabine

Gemcitabine (LY188011) 是一种人工合成的胞嘧啶核苷衍生物，一种 DNA 合成抑制剂。Gemcitabine 具有抗肿瘤活性和抗代谢活性。Gemcitabine 可以引起细胞自噬和凋亡。

Gemcitabine monophosphate is a novel HDAC inhibitor with broad-spectrum antitumor activity against solid (IC50: 30 to 300 nM) and hematological malignancies. Gemcitabine monophosphate was found to be a potent inhibitor of HDAC1 and -8 (class I) in vitro.

Gemcitabine elaidate (CP-4126) 是 Gemcitabine 的亲脂性前药。它通过酯酶转化为 Gemcitabine 以被磷酸化。它具有抗肿瘤活性。

LY2334737 是一种具有口服活性的 Gemcitabine 的前药，也是核苷类似物。它抑制肠道病毒 A71 感染，有抗病毒和抗癌活性。

Mc-O- Si(di-iso)-O-Gemcitabine 是一种硫醇反应型 Drug-linker,可用于抗体-药物偶联物（ADC）的合成。

Gemcitabine elaidate (CP-4126) hydrochloride 是 Gemcitabine 的亲脂性前药。Gemcitabine elaidate hydrochloride 通过酯酶转化为 Gemcitabine 以被磷酸化。Gemcitabine elaidate hydrochloride 可以口服给药，具有抗肿瘤活性。

Gemcitabine-O-Si(di-iso)-O-Mc, a drug-linker conjugate for Antibody-Drug Conjugates (ADC), exhibits potent antitumor activity. It incorporates Gemcitabine, a pyrimidine nucleoside analog antimetabolite and antineoplastic agent, connected through the ADC linker[1].

Gemcitabine triphosphate (dFdCTP) 是 Gemcitabine 在细胞内的两种核苷代谢产物的一种。另一种是活性二磷酸 (dFdDTP)。Gemcitabine triphosphate 能够作为放射性标记探针成像研究的标准物，用于识别对 Gemcitabine 的肿瘤，并评估 Gemcitabine 被细胞摄取和保留性质。

Gemcitabine hydrochloride (LY 188011 hydrochloride) 是一种人工合成的胞嘧啶核苷衍生物，一种 DNA 合成抑制剂。Gemcitabine 具有抗肿瘤活性和抗代谢活性。Gemcitabine 可以引起细胞自噬和凋亡。

Gemcitabine EP Impurity C-13C-15N2 是 Gemcitabine EP Impurity C 的 13C 和 15 N 的标记化合物。

Gemcitabine monophosphate sodium salt hydrate 是Gemcitabine 的单磷酸盐衍生物。

dFdCTP trisodium (Gemcitabine triphosphate trisodium) 是 Gemcitabine 衍生物，具有细胞毒性，抑制 DNA 合成所需的过程。dFdCTP trisodium 抑制 T-araCTP 和 araCTP，可掺入 DNA 并终止 DNA 链延伸。

AFMK (Formyl-N-acetyl-5-methoxykynurenamine) 是褪黑激素的活性代谢物，具有抗氧化和自由基清除活性。 AFMK 是一种凋亡调节剂，可提高吉西他滨在 PANC-1 细胞中的抗肿瘤作用。

2'-Deoxycytidine hydrochloride（2'-脱氧胞苷盐酸盐）是2'-Deoxycytidine的盐酸盐形式，是一种重要的脱氧核糖核苷类似物，常用于DNA合成且具有潜在的抗癌作用，其衍生物Gemcitabine已被开发为抗癌药物。2'-Deoxycytidine hydrochloride使小鼠能够免受阿糖胞苷（araC）的致死毒性。

GNE-900 是一种 ATP 竞争性、选择性和口服活性 ChK1抑制剂，对 ChKl,ChK2的 IC50值分别为为 0.0011，1.5 µM。GNE-900 废除 G2-M 检查点，增强 DNA 损伤，并诱导胞凋亡 (Apoptosis)。gemcitabine 和 GNE-900 给药显示抗肿瘤活性[1]< sup>。

Pixatimod（又名PG-545）是一种合成的改性糖类肝素硫酸模拟剂及Toll样受体9（TLR9）的激动剂，具有潜在的免疫刺激、抗肿瘤和抗病毒活性。Pixatimod强效抑制SARS-CoV-2，其通过破坏刺突蛋白-ACE2的相互作用来实现。此外，Pixatimod阻断了多种促癌过程，包括细胞增殖、侵袭、转移、血管生成及上皮-间充质转换。这些活性在多种不同的小鼠癌症模型中显示出强大效果，涵盖约30种异种移植模型和20种同源移植模型。Pixatimod已与多种已获批准的抗癌化合物联合测试，展现其临床潜力，包括与吉西他滨、紫杉醇、索拉非尼、铂类化合物和一种抗PD-1抗体的联合应用。

DSPE-PEG(2000)-amine is a PEGylated derivative of 1,2-distearoyl-sn-glycero-3-PE . It has been used in the synthesis of solid lipid and thermosensitive liposomal nanoparticles for the delivery of anticancer agents.1,2,3DSPE-PEG(2000)-amine has also been used in the synthesis of fluorescein isothiocyanate-loaded mesoporous silica nanoparticles for imaging applications.4It can be conjugated to a variety of functional molecules for improved cellular targeting and uptake of DSPE-PEG(2000)-amine-containing nanoparticles.4,5 1.Sloat, B.R., Sandoval, M.A., Li, D., et al.In vitro and in vivo anti-tumor activities of a gemcitabine derivative carried by nanoparticlesInt. J. Pharm.409(1-2)278-288(2011) 2.Abd-Rabou, A.A., Bharali, D.J., and Mousa, S.A.Taribavirin and 5-fluorouracil-loaded pegylated-lipid nanoparticle synthesis, p38 docking, and antiproliferative effects on MCF-7 breast cancerPharm. Res.35(4)76(2018) 3.Affram, K., Udofot, O., Singh, M., et al.Smart thermosensitive liposomes for effective solid tumor therapy and in vivo imagingPLoS One12(9):e0815116(2017) 4.Wang, L.-S., Wu, L.-C., Lu, S.-Y., et al.Biofunctionalized phospholipid-capped mesoporous silica nanoshuttles for targeted drug delivery: Improved water suspensibility and decreased nonspecific protein bindingACS Nano4(8)4371-4379(2010) 5.Wen, X., Wang, K., Zhao, Z., et al.Brain-targeted delivery of trans-activating transcriptor-conjugated magnetic PLGA lipid nanoparticlesPLoS One9(9):e106652(2014)

FF-10502 is a pyrimidine nucleoside antimetabolite and a structural analog of Gemcitabine. This compound effectively inhibits DNA polymerase α and β, demonstrating potent anticancer activity by targeting dormant cells.

TC113是一种与c(RGDyK)偶联的Gemcitabine。它通过整合素αvβ3可被A549细胞内化。此外，TC113对WM266.4和A549细胞表现出显著的抗增殖效果。

PD-321852 is a small-molecule Chk1 inhibitor, which potentiates gemcitabine-induced clonogenic death in a panel of pancreatic cancer cell lines and evaluated the relationship between endpoints associated with Chk1 inhibition and chemosensitization. Gemcitabine chemosensitization by minimally toxic concentrations of PD-321852 ranged from minimal (<3-fold change in survival) in Panc1 cells to >30-fold in MiaPaCa2 cells. PD-321852 inhibited Chk1 in all cell lines as evidenced by stabilization of Cdc25A; in combination with gemcitabine, a synergistic loss of Chk1 protein was observed in the more sensitized cell lines.

Tetrahydrouridine (NSC-112907; THU) 是一种多药耐药调节剂。它可用于癌症治疗，使肿瘤细胞对放射治疗更加敏感。 它是一种竞争性胞苷脱氨酶 (CDA) 抑制剂，可抑制 ara-C 和吉西他滨等细胞毒性脱氧胞苷类似物分解代谢中的脱氨作用。

Troxacitabine, a DNA polymerase inhibitor, is potentially used for the treatment of acute myeloid leukemia (AML). In comparison with gemcitabine, troxacitabine was equally active against MiaPaCa and was more efficacious against Panc-01.

Vactosertib Hydrochloride (EW-7197 Hydrochloride) 是一种具有口服活性和高效性的 ATP 竞争性激活素受体样激酶 5 (ALK5) 抑制剂，是 TGF-β 受体 I 抑制剂，具有抗转移活性和抗癌作用，通过协同抑制胰腺癌细胞的活力使胰腺癌细胞对吉西他滨敏感。

SL-01 is an oral derivative of gemcitabine. SL-01 inhibited human breast cancer growth through the induction of apoptosis. SL-01 inhibited human cancer growth more potently than gemcitabine.