T82327
|
|
|
|
GEM–IB是一种由吉西他滨(GEM)-5'-磷酸与伊班膦酸盐(IB)组成的复合物。在小鼠骨肉瘤(OS)模型中,GEM–IB能够作为独立活性分子减轻肿瘤负担,并在与多西紫杉醇(DTX)联合使用时,能进一步保护骨结构并提高生存率。 |
T74400
|
|
|
|
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。 |
T17175
|
|
|
Others
|
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. |
T18313
|
|
|
Others
|
Mc-O-Si(di-iso)-Cl is a cleavable ADC linker, commonly employed in the synthesis of antibody-drug conjugates (ADCs) like Gemcitabine-O-Si(di-iso)-O-Mc [1]. |
T74765
|
|
|
|
Viral polymerase-IN-1 hydrochloride 是一种 Gemcitabine 衍生物,有效抑制甲型和乙型流感病毒 (influenza) 感染,IC90值为 11.4-15.9 μM。Viral polymerase-IN-1 hydrochloride 对 SARS-CoV-2感染具有活性。Viral polymerase-IN-1 hydrochloride 通过影响细胞中的病毒 RNA 复制/转录来抑制流感病毒感染。 |
T63074
|
|
|
|
Ivaltinostat (CG-200745) formic 是一种口服具有活力的泛 HDAC 抑制剂,具有异羟肟酸部分,能够在催化袋底部结合锌。Ivaltinostat formic 对组蛋白 H3 和微管蛋白的脱乙酰作用具有抑制效果。Ivaltinostat formic 能够促使 p53 的积累,诱导 p53 依赖性反式激活,并提高 MDM2 和 p21 (Waf1/Cip1) 蛋白的表达。Ivaltinostat formic 增加 Gemcitabine 耐药细胞对 Gemcitabine 和 5-Fluorouracil (5-FU) 的敏感性。Ivaltinostat formic 诱导凋亡,并具有抗肿瘤效果。 |
T18369
|
|
|
Others
|
N-(5-Hydroxypentyl)maleimide is a non-cleavable ADC linker, commonly employed in the synthesis of antibody-drug conjugates (ADCs). It serves as a crucial component in the production of Gemcitabine-O-Si(di-iso)-O-Mc, an ADC compound [1]. |
T74530
|
|
|
|
GEM-5为基于吉西他滨且含HIF-1α抑制剂(YC-1)的偶联物,IC50值为30 nM。此化合物能有效降低HIF-1α表达,并提高肿瘤抑制因子p53的表达量。GEM-5可诱导A2780细胞的凋亡(apoptosis),进而抑制肿瘤生长。 |
T36103
|
|
|
|
TW9 is a dual inhibitor of bromodomain 2 (BD2) in bromodomain-containing protein 4 (BRD4) and histone deacetylase 1 (HDAC1; IC50s = 0.074 and 0.29 μM, respectively).1It is selective for BD2 over BD1 in BRD4 (IC50= 0.72 μM) and for HDAC1 over HDAC2 (IC50= 2.5 μM). TW9 (50 nM) induces apoptosis in, and inhibits proliferation of, MIA PaCa-2 pancreatic cancer cells. It induces cell cycle arrest at the G1phase in HPAC pancreatic cancer cells when used at a concentration of 2 μM. TW9 acts synergistically with gemcitabine to reduce the viability of HPAC cells.
1.Zhang, X., Zegar, T., Weiser, T., et al.Characterization of a dual BET/HDAC inhibitor for treatment of pancreatic ductal adenocarcinomaInt. J. Cancer147(10)2847-2861(2020) |
T17059
|
|
|
DNA Methyltransferase
|
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。 |