cytarabine

Cytarabine (Ara-C) 是一种核苷类似物，一种 DNA 合成抑制剂 (IC50=16 nM)。Cytarabine 可以抑制 DNA 聚合酶，诱导细胞周期阻滞、细胞自噬和凋亡。Cytarabine 具有抗肿瘤活性。

Cytarabine triphosphate (Ara-CTP), a competitive inhibitor of DNA synthesis and an active metabolite of Cytarabine, exhibits predictive potential for leukemic blasts' chemosensitivity to Cytarabine through intracellular levels.

Cytarabine 5′-monophosphate (ara-CMP), an active metabolite of the nucleoside analog cytarabine formed by deoxycytidine kinase, is incorporated into DNA by DNA polymerase α, significantly slowing DNA synthesis. It inhibits nuclear and mitochondrial DNA replication in S. cerevisiae at 15 mM and improves survival in an L1210 murine leukemia model at 3.5-75.1 mg kg.

Cytarabine triphosphate (Ara-CTP) trisodium 是 Cytarabine 的活性代谢物，为 DNA 合成的竞争性抑制剂。细胞内 Cytarabine triphosphate trisodium 的水平可预测白血病母细胞对 Cytarabine 的化学敏感性。

Cytarabine hydrochloride (Ara-C hydrochloride) 是一种核苷类似物，可导致 S 期细胞周期停滞并抑制DNA 聚合酶。Cytarabine 抑制DNA 合成，IC50为 16 nM。Cytarabine hydrochloride 对HSV 具有抗病毒作用。

Elacytarabine (M7594 0037) 是核苷类似物阿糖胞苷的一种脂质缀合衍生物。Elacytarabine (M7594 0037) (CP 4055) 是一种抗肿瘤药物，在实体瘤中具有细胞毒性。

Adamantoylcytarabine is abioactive chemical.

CPX-351 (Vyxeos) 是阿糖胞苷和柔红霉素的脂质体封装物，具有潜在的抗肿瘤活性，可用与研究急性髓系白血病。

MBC-11 通过将阿糖胞苷和依替膦酸盐浓缩在疾病部位来靶向癌症的偶联物。MBC-11 可溶用于研究肿瘤诱发的骨病。

Flurocitabine HCl 是阿糖胞苷的氟化酸酐类似物，在体内部分水解成两种活性抗肿瘤物质 (阿拉伯糖基-氟尿嘧啶 (ara-FC) 和阿拉伯糖基-氟尿嘧啶 (ara-FU))。Flurocitabine HCl 在急性白血病和实体瘤的 I 期研究中具显示出抗肿瘤活性。

Retinoic acid (Tretinoin) 是维生素 A 的代谢产物，是一种视黄酸受体 RAR 的天然激动剂，激动 RARα β γ (IC50=14 nM)。Retinoic acid 可以诱导细胞分化、减少细胞增殖和抑制肿瘤发生。

Ancitabine hydrochloride (NSC 145668 HCl) 是一种天然的抗白血病药物。

MBC-11 triethylamine has potential to treat tumor-induced bone disease (TIBD), is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC).

Fosteabine is an oral and prodrug analog of cytarabine. It is resistant to deoxycytidine deaminase.

Ancitabine, a congener of cyterabine, is metabolized to cytarabine, thereby maintains a more constant antineoplastic action.

Prostratin(12-Deoxyphorbol-13-acetate，13-O-乙酰基-12-脱氧佛波醇)是一种具有口服活性的蛋白激酶C（PKC）激活剂，Ki值为12.5 nM。作为一种NF-κB激活剂，Prostratin可激活T细胞中HIV基因的表达。Prostratin能抑制急性髓系白血病（AML）细胞系的生长，并增强阿糖胞苷诱导的AML细胞分化。此外，Prostratin诱导KRAS磷酸化并抑制KRAS突变的肿瘤生长。

Fazarabine, also known as Kymarabine, is an orally-active pyrimidine analogue of an aza-substituted cytidine in which the ribose moiety is replaced by an arabinose sugar. Similar in action to cytarabine, fazarabine is phosphorylated by deoxycytidine kinase to a triphosphate form which competes with thymidine for incorporation into DNA; its incorporation into DNA inhibits DNA synthesis, resulting in tumor cell death and tumor necrosis. The presence of deoxycytidine kinase in a tumor is a determinant of tumor sensitivity to this drug.

APcK110 is a novel Kit inhibitor . APcK110 inhibits proliferation of the mastocytosis cell line HMC1.2 and the SCF-responsive cell line OCI AML3 in a dose-dependent manner . APcK110 is a more potent inhibitor of OCI AML3 proliferation than the clinically used Kit inhibitors imatinib and dasatinib and at least as potent as cytarabine. APcK110 inhibits the phosphorylation of Kit, Stat3, Stat5, and Akt in a dose-dependent fashion, showing activity of APcK110 on Kit and its downstream signaling pathways . APcK110 may have potent application in AML.

Ara-SH为Cytarabine巯基丙酸取代的衍生物，应用于通过自组装技术制造携带Cytarabine和Venetoclax的智能共负载纳米颗粒(AV-NP)的触发器。在体外和体内实验中，Ara-SH展现出显著的协同抗白血病效果。