1. Cell Cycle/DNA Damage Cytoskeleton
  2. Microtubule/Tubulin
  3. IKP-104

IKP-104 是一种微管/微管蛋白 (microtubule/tubulin) 抑制剂 (IC50 = 1.31 μM) 。IKP-104 通过抑制微管 (microtubule) 合和诱导细胞骨架微管 (microtubule) 解聚来阻止细胞处于有丝分裂期和 M 期。IKP-104 抑制小鼠和人类肿瘤细胞系的生长。IKP-104 对小鼠腹水瘤以及肺癌模型具有抗肿瘤作用。IKP-104 可用于白血病、肺癌、黑色素瘤等癌症的研究。

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IKP-104

IKP-104 Chemical Structure

CAS No. : 114231-14-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IKP-104 is a microtubule/tubulin inhibitor (IC50 = 1.31 μM). IKP-104 arrests cells in mitosis and the M phase by inhibiting microtubule polymerization and inducing cytoskeletal microtubule depolymerization. IKP-104 inhibits the growth of mouse and human tumor cell lines. IKP-104 exhibits anti-tumor effects in mouse ascites tumors and lung cancer models. IKP-104 is useful in the research of cancers such as leukemia, lung cancer and melanoma[1][2][3][4].

体外研究
(In Vitro)

IKP-104 (0-25 μM) 可抑制 tau 诱导的未分级微管蛋白以及同型纯 αβII 和 αβIV 的聚合,但对 αβIII 无影响[1]
IKP-104 (1.5 μM) 可迫使大量预先形成的微管形成聚集体 (未分级微管蛋白和 αβIII) 和螺旋体 (αβII 同型),但对由 αβIV 形成的微管的形态无影响[1]
KP-104 (0-40 μM,0-40 分钟) 可增加吸光度,改变聚集体的形成和现有微管的形态[1]
KP-104 对 L1210、B16、Lewis、K562、HeLa 细胞有细胞毒性,IC50 分别为 0.0025、5.2、0.0017、0.0012、0.015 μg/mL[2]
KP-104 (3.6 μg/mL,0-48 小时) 通过抑制 B16 细胞中细胞骨架微管的聚合和诱导微管的解聚,增加圆形细胞的比例,使细胞停滞在 M 期和有丝分裂期[2][3]

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

Cell Cycle Analysis[2][3]

Cell Line: B16 cells
Concentration: 3.6 μg/mL
Incubation Time: 0, 1, 3, 6, 9, 12, 24 and 48 h
Result: Increased the proportion of round-shaped cells, arrested cells in G1-M phase, and induced polyploid and multinuclear.
Accumulated mitotic cells, and the Ml.
Caused the fine reticular microtubule network of prophase cells to disappear, resulting in a single mitotic spindle during metaphase, shortened the centromere microtubules during anaphase and telophase, and the early interphase microtubule network to re-form after cell division.
Depolymerized spindle microtubules in mitotic cells, but no changes in the microtubule network were observed in interphase cells after 20 minutes of exposure.
Caused the microtubule network of interphase cells to gradually disappear after 2 h of treatment, weak fluorescence appears in the cytoplasm of mitotic and interphase cells, accompanied by a small amount of microtubule fragments.
Resulted the induction of bundles of varying sizes composed of numerous wavy protofilaments at 2 and 24 h.
体内研究
(In Vivo)

IKP-104 (0.5-5 mg/kg,腹腔/皮下注射,每日一次,5-9 天) 在小鼠腹水肿瘤和小鼠 Lewis 肺癌模型中显示出抗肿瘤活性[2]

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

Animal Model: CDF1 murine ascetic tumor (L1210, 1x105) model[2]
Dosage: 0.5 mg/kg, 1 mg/kg, 5 mg/kg
Administration: i.p., once a day, 5 days
Result: Showed antitumor activity, at doses of 1.0 and 5.0 mg/kg showed effects com-parable to those of 5-Fluorouracil (HY-90006) at 10.0 and 20.0 mg/kg andvindesine at 0.3 mg/kg.
Animal Model: C57BL/6 murine Lewis (1x105) lung carcinoma model[2]
Dosage: 1 mg/kg, 5 mg/kg
Administration: s.c., once a day, 9 days
Result: Showed antitumor activity.
分子量

449.90

Formula

C26H21ClFNO3

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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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    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:
IKP-104
目录号:
HY-W854934
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