2. Cell Cycle/DNA Damage Cytoskeleton
  3. Mps1
  4. CFI-401870

CFI-401870 是一种口服有效的苏氨酸酪氨酸激酶 (TKK (Mps1)) 抑制剂，其 IC50 为 3.1 nM。CFI-401870 对 PLK4、KDR、AURKA 以及其他激酶 (例如 AURKB/INCENP) 的 IC50 均大于 1 μM。CFI-401870 可抑制多种癌细胞的生长，导致染色体滞后、非整倍体增加和细胞周期阻滞。CFI-401870 可用于结肠癌等癌症的研究。

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CFI-401870

CFI-401870 Chemical Structure

CAS No. : 1430741-35-7

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CFI-401870 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CFI-401870 is an orally active threonine tyrosine kinase (TKK (Mps1)) inhibitor with an IC50 of 3.1 nM. CFI-401870 exhibits IC50s against PLK4, KDR, AURKA and other kinases such as AURKB/INCENP were all greater than 1 μM.CFI-401870 inhibits the growth of various cancer cells, causing chromosome lag, an increase in aneuploidy and cell cycle arrest. CFI-401870 can be used for the study of cancers such as colon cancer[1].

体外研究
(In Vitro)

CFI-401870 抑制 MDA-MB-468、HCT-116 和 OVCAR-3 细胞增殖，其 GI50 分别为 36、17 和 80 nM[1]。
CFI-401870 (0.05-3 μM，48 小时) 以浓度依赖的方式诱导 G2/M 期阻滞，并伴有 HCT116 细胞中多倍体细胞比例的显著增加[1]。
CFI-401870 (0.1-0.5 μM，6-28 小时) 导致 HCT116 细胞染色体排列异常和纺锤体检查点缺陷[1]。

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

CFI-401870 相关抗体:

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.05, 0.1, 0.2, 0.5, 1 and 3 μM
Incubation Time: 48 h
Result: Induced G2/M phase arrest in a concentration-dependent manner.
体内研究
(In Vivo)

CFI-401870 (23-35 mg/kg，口服，每日一次，持续 21 天) 在多种异种移植小鼠模型 (包括 HCT116 结肠癌、MDA-MB-468 乳腺癌和 SW48 结肠癌) 中均表现出显著的抗肿瘤活性[1]。

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

Animal Model: HCT116 colon cancer model established in female CD-1 nude mice[1]
Dosage: 23 and 35 mg/kg
Administration: Oral administration (p.o.), once daily for 21 days
Result: Exhibited 77% and 55% tumor growth inhibition (TGI) for 75 at 35 and 23 mg/kg, respectively.
分子量

493.60

Formula

C30H31N5O2
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

CFI-401870 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

CFI-4018701430741-35-7CFI401870CFI 401870Mps1Monopolar spindle 1Mps1 kinaseindazole carboxamidesstructure-activity relationshipanticancer agentscell cycle checkpointInhibitorinhibitorinhibit

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