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IH2120 (±)-10-羟基喜树碱 抑制剂/拮抗剂/激动

剂 索莱宝
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  • ¥590
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  • 北京
  • IH2120
  • 2025年07月23日
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    • 详细信息
    • 文献和实验
    • 技术资料
    • 保存条件

      Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year

    • 保质期

      Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year

    • 英文名

      (±)-10-Hydroxycamptothecin

    • 库存

      现询

    • 供应商

      北京索莱宝科技有限公司

    • CAS号

      64439-81-2

    • 规格

      25mg

    【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】

    标题:Crotonylation of MCM6 enhances chemotherapeutics sensitivity of breast cancer via inducing DNA replication stress

    成员:Haoyun Song, Zhao Guo, Kun Xie, Xiangwen Liu, Xuguang Yang, Rong Shen, Degui Wang

    论文因子:5.9 发表期刊:CELL PROLIFERATION pmid:39477811

    基本信息
    CASNo.64439-81-2
    中文名称(±)-10-羟基喜树碱
    英文名称(±)-10-Hydroxycamptothecin
    分子式C20H16N2O5
    分子量364.35
    溶解性Soluble in DMSO ≥3mg/mL(Need ultrasonic)
    纯度≥98%
    外观(性状)Light yellow to yellow Solid
    储存条件Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
    ECEINECS 613-598-9
    MDLMFCD00274425
    SMILESCCC1(C2=C(COC1=O)C(=O)N3CC4=C(C3=C2)N=C5C=CC(=CC5=C4)O)O
    InChIKeyHAWSQZCWOQZXHI-UHFFFAOYSA-N
    InChIInChI=1S/C20H16N2O5/c1-2-20(26)14-7-16-17-11(5-10-6-12(23)3-4-15(10)21-17)8-22(16)18(24)13(14)9-27-19(20)25/h3-7,23,26H,2,8-9H2,1H3
    PubChem CID4330531
    靶点Topoisomerase
    通路DNA Damage/DNA Repair
    背景说明(±)-10-Hydroxycamptothecin 是一种生物碱,能够抑制拓扑异构酶 I (topoisomerase I) 的活性,具有广谱的抗肿瘤活性。
    生物活性(±)-10-Hydroxycamptothecin is an indole alkaloid that inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity.[1-3]
    In Vitro(±)-10-Hydroxycamptothecin (10-OH-camptothecin) is an inhibitor of topo I[1]. (±)-10-Hydroxycamptothecin (10-HCPT, 5-20 nM) markedly inhibits the proliferation of Colo 205 cells in a dose-dependent manner. (±)-10-Hydroxycamptothecin (5-20 nM) arrests Colo 205 cells in the G2 phase of the cell cycle and triggers apoptosis through a caspase-3-dependent pathway[2]. (±)-10-Hydroxycamptothecin (HPT, 0.01-10 μg/mL) causes cell shrinage, nuclear fragmentation and condensed chromosomes and induces apoptosis of human urinary bladder cancer cell line (T24)[3].
    细胞实验(±)-10-Hydroxycamptothecin (10-HCPT, 2.5-7.5 mg/kg/2 days, p.o.) significantly suppresss tumor growth in mouse xenografts. (±)-10-Hydroxycamptothecin (1-7.5 mg/kg, p.o., once per 2 or 4 days) causes no obvious acute toxicity in nude mice[2].
    细胞实验Colo 205 cells (5 × 105) (ATCC: CCL-222) are seeded in 25T flasks overnight and then treated without (control) and with 5, 10, 15 or 20 nM of (±)-10-Hydroxycamptothecin, respectively. After treatment for 24-120 h, cells are harvested by trypsin-EDTA and then centrifuged at 1,500 rpm for 5 min at 4?C. The cell pellet is resuspended in culture medium containing 0.04% trypan blue and the viable cells are enumerated by a hemocytometer[2].
    动物实验BALB/c-nu mice are housed in a laminar flow room under sterilized conditions with a maintained temperature of 25 ± 2?C and a controlled 12-h light and 12-h dark cycle. The Colo 205 cells are harvested and resuspended in serum-free RPMI-1640 medium. Cells are adjusted to 1 × 107 cells/mL, and transplanted 0.1 mL subcutaneously to the flank regions of the mice. Each experimental group included six to seven mice bearing tumors. (±)-10-Hydroxycamptothecin is dissolved in propylene glycol and treatment begins when the tumor size reach 3-5 mm. (±)-10-Hydroxycamptothecin is administered via p.o. once per two or four days at doses of 1, 2.5, 5, 7.5 mg/kg (volume of injection: 0.1 mL/20 g of body weight), respectively. The control group receives propylene glycol vehicle once per two days. Tumor size and body weight are monitored twice a week throughout the experiment. The tumor size is measured using a vernier caliper. Tumor volume (V) is calculated according to the formula: V (mm3) = 0.4AB2, where A and B are the longest diameter and the shortest diameter, respectively. At the end of the experiment, all mice are sacrificed by CO2 gas. Tumors, livers, kidneys and lungs are collected, fixed, embedded and stained with hematoxylin and eosin for pathological analysis[2].
    数据来源文献[1]. Liu SY, et al. Interaction of several nucleoside triphosphate analogues and 10-hydroxycamptothecin with human DNA topoisomerases. Cancer Res. 1989 Mar 15;49(6):1366-70.
    [2]. Ping YH, et al. Anticancer effects of low-dose 10-hydroxycamptothecin in human colon cancer. Oncol Rep. 2006 May;15(5):1273-9.
    [3]. Fan J, et al. Detection of apoptosis exposed to 10-hydroxycamptothecin in T24 human urinary bladder cancer cells. Zhonghua Wai Ke Za Zhi. 1999 Jan;37(1):57-9.
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    【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】

    标题:Crotonylation of MCM6 enhances chemotherapeutics sensitivity of breast cancer via inducing DNA replication stress

    成员:Haoyun Song, Zhao Guo, Kun Xie, Xiangwen Liu, Xuguang Yang, Rong Shen, Degui Wang

    论文因子:5.9 发表期刊:CELL PROLIFERATION pmid:39477811

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