1. Cell Cycle/DNA Damage
  2. Topoisomerase DNA/RNA Synthesis
  3. F-14512 hydrochloride

F-14512 hydrochloride 是一种抗癌剂,利用多胺转运系统 (PTS) 将含多胺的药物选择性地输送至癌细胞。F-14512 hydrochloride 通过多胺与 DNA 的亲和力增强拓扑异构酶 II (topoisomerase II) 抑制,并实现了选择性细胞摄取。F-14512 hydrochloride 对 PTS 活性高的细胞表现出显著的细胞毒性,并诱导了 DNA 损伤。F-14512 hydrochloride 在 MX1 乳腺肿瘤异种移植模型中,表现出强效的抗肿瘤活性。F-14512 hydrochloride 可用于研究乳腺癌。

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F-14512 hydrochloride

F-14512 hydrochloride Chemical Structure

CAS No. : 866874-39-7

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  • 参考文献

生物活性

F-14512 hydrochloride is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 hydrochloride enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 hydrochloride exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 hydrochloride demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 hydrochloride could be used to study breast cancer[1].

体外研究
(In Vitro)

F-14512 (0.001-100 μM) hydrochloride 通过多胺转运系统进入细胞。在具有正常 PTS 的 CHO 细胞中,IC50 为 0.12 μM;而在 PTS 缺陷的 CHO-MG 细胞中,IC50 为 8.7 μM[1]
F-14512 (72 h) hydrochloride 在多种人类细胞系中表现出高效性 (中位 IC50 = 0.18 μM),尤其对 MX-1、LOX-IMV1 和 HL-60 等细胞系有效[1]
F-14512 (1-100 μM,1-24 h) hydrochloride 可诱导 A549 细胞 DNA 损伤,并在具有 DNA 缺陷的 xrs6 细胞中表现出更强的细胞毒性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

F-14512 (0.16-1.25 mg/kg,腹腔注射,每日一次,持续 2 周) hydrochloride 在 MX-1 模型中表现出优异的抗肿瘤活性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MX-1 human breast cancer xenograft model established in homozygous female athymic nude mice[1]
Dosage: 0.16, 0.32, 0.63, 1.25 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 2 weeks
Result: Led to tumor regression dose-dependently.
分子量

787.60

Formula

C33H51Cl4N5O8

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
F-14512 hydrochloride
目录号:
HY-106031A
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