T4060
|
|
|
DNA/RNA Synthesis
|
Acelarin (NUC-1031) 是核苷类似物吉西他滨的 ProTide 改造和增强产品。 |
T67291
|
|
|
Drug Metabolite
|
2′,2′-Difluorodeoxyuridine (dFdU) 是 Gemcitabine 的主要代谢产物。2′,2′-Difluorodeoxyuridine 具有抗癌和抗肿瘤活性,在低氧条件下的显示出放射增敏作用,可用于研究胰腺癌。 |
T41345
|
|
|
Apoptosis
Free radical scavengers
Antioxidant
Endogenous Metabolite
|
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。 |
T16813
|
|
|
Nucleoside Antimetabolite/Analog
|
RX-3117 (fluorocyclopentenylcytosine) 是一种新型的胞苷类似物,在几种癌细胞系中显示出抗癌活性,包括对吉西他滨耐药的变体。 |
T4126
|
|
|
NF-κB
p53
|
CBL0137 (Curaxin 137) 是一种代谢稳定的 curaxin,可激活 p53 (EC50: 0.37 μM) 并抑制 NF-κB (EC50: 0.47 μM)。它在功能上使促进染色质转录复合物 (FACT) 失活,从而驱动对 p53 和 NF-κB 的影响并促进癌细胞死亡。口服 CBL0137 在小鼠体内具有广泛的抗癌活性,可根除耐药性癌症干细胞,并增强吉西他滨在胰腺癌临床前模型中的疗效。 |
T71259
|
|
|
Apoptosis
Chk
|
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>。 |
T68981
|
|
|
|
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. |
T19779
|
|
|
|
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. |
T79198
|
|
|
Nucleoside Antimetabolite/Analog
|
S-Gem为TrxR依赖性前药,是Gemcitabine的衍生物,能够被TrxR选择性激活。与Gemcitabine相比,S-Gem展现出较低的细胞毒性。 |
T39290
|
|
|
|
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. |