2. Cell Cycle/DNA Damage Neuronal Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. Polo-like Kinase (PLK) Trk Receptor Apoptosis
  4. CZS-241

CZS-241 是一种口服有效的选择性 Polo-like Kinase (PLK) 4 抑制剂 (IC50=2.6 nM)。CZS-241 还抑制 TRKA，IC50 值为 2.74 μM。CZS-241 诱导细胞凋亡 (apoptosis)，阻滞细胞周期在 S/G2 期。CZS-241 对白血病细胞系表现出高效的抗增殖活性，对正常细胞系表现出安全性。

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CZS-241 Chemical Structure

CZS-241 Chemical Structure

CAS No. : 3016297-55-2

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CZS-241 相关抗体

Top Publications Citing Use of Products

查看 Polo-like Kinase (PLK) 亚型特异性产品:

查看所有亚型
PLK1 PLK2 PLK3 PLK4

查看 Trk Receptor 亚型特异性产品:

查看所有亚型
TrkA TrkB TrkC Trk

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CZS-241 is an orally active and selective inhibitor of Polo-like Kinase (PLK) 4 (IC50=2.6 nM). CZS-241 inhibits TRKA with an IC50 value of 2.74 μM. CZS-241 induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines[1].

IC50 & Target[1]

PLK4

2.6 nM (IC50)

TrkA

2.74 μM (IC50)

体外研究
(In Vitro)

CZS-241 抑制慢性粒细胞白血病 (CML) 细胞系 K562 和 KU-812 的细胞增殖，IC50 分别为 0.096 μM 和 0.25 μM。CZS-241 对包括 HUVEC 和 L02 在内的正常细胞影响很小[1]。
CZS-241 (10 μM；0-120 分钟) 在人肝微粒体中表现出 31.5 分钟的半衰期 t1/2 和 41.8 μL/min/kg 的 CLint[1]。
CZS-241 (0.3 μM、1 μM、3 μM；48 小时) 使细胞周期停滞在 S/G2 期，并诱导 K562 CML 细胞凋亡[1]。
CZS-241 (0.03-0.3 μM) 在 K562 细胞中抑制 PLK4 磷酸化，增加 FBXW5 表达水平但降低 SAS-6 表达水平[1]。

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

CZS-241 相关抗体:

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 0.03 μM, 0.1 μM, 0.3 μM, 1 μM, and 3 μM
Incubation Time:
Result: Showed insignificant effect on PLK4 relative expression, but decreased the expression of SAS-6 dose-dependently.
Increased the expression level of FBXW5.
体内研究
(In Vivo)

CZS-241（30 mg/kg；口服；单剂量）在小鼠体内显示出超过 4 小时的半衰期和 70.8% 的生物利用度[1]。
CZS-241（20 mg/kg/天；口服；21 天）在 K562 细胞异种移植小鼠模型中显着抑制肿瘤进展[1]。
CZS-241（200 mg/kg；口服；单剂量）对小鼠的心脏、肝脏、脾脏、肺和肾脏，在检测的 7 天内没有明显的毒性迹象[1]。

在小鼠中的药代动力学分析[1]

Route Dose (mg/kg) AUClast (ng·h/mL) AUCINF_obs (ng·h/mL) t1/2 (h) Tmax (h) Cmax (ng/mL) Clobs (L·h/kg) Vss_obs (mL/kg) MRTINF_obs (h) F (%)
i.v. 3 727 739 2.15 / / 68.7 12615 1.28 70.8
p.o. 30 5177 5231 4.13 0.67 1880 / / 3.87 /

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

Animal Model: K562 cells xenograft mouse model[1]
Dosage: 10 mg/kg, 20 mg/kg
Administration: PO; once daily, for continuous 21 days
Result: Showed potent antitumor activity with mouse body weight increased normally. Exhibited tumor growth inhibition (TGI) rate of 56.4% at 20 mg/kg/day dosage.
分子量

551.98

Formula

C26H24ClF2N9O
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

CZS-241 相关分类

  • 摩尔计算器

  • 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.

Keywords:

CZS-2413016297-55-2CZS241CZS 241Polo-like Kinase (PLK)Trk ReceptorApoptosisTropomyosin related kinase receptor Inhibitorinhibitorinhibit

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