1. Cell Cycle/DNA Damage Cytoskeleton
  2. Mps1
  3. TTK-IN-5

TTK-IN-5 是一种口服有效、有选择性的共价苏氨酸酪氨酸激酶 (TTK) 抑制剂 (IC50 = 8.918 nM)。TTK-IN-5 对 MDA-MB-231、A2780、HCT116、HCC1569 和 MKN1 细胞系均表现出抗增殖活性,IC50 值分别为 0.113 μM、0.476 μM、3.136 μM、3.649 μM 和 1.856 μM。在 A2780 和 MDA-MB-231 异种移植小鼠模型中,TTK-IN-5 能有效抑制肿瘤生长且无明显毒性。TTK-IN-5 可用于乳腺癌和卵巢癌等癌症的研究。

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TTK-IN-5

TTK-IN-5 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TTK-IN-5 is an orally active covalent threonine tyrosine kinase (TTK) inhibitor with selectivity (IC50 = 8.918 nM). TTK-IN-5 exhibits anti-proliferative potencies against MDA-MB-231, A2780, HCT116, HCC1569 and MKN1 cell lines (IC50 values of 0.113 μM, 0.476 μM, 3.136 μM, 3.649 μM, and 1.856 μM, respectively). TTK-IN-5 potently suppresses tumor growth without notable toxicity in A2780 and MDA-MB-231 xenograft mouse models. TTK-IN-5 can be used for the research of cancer such as breast cancer and ovarian cancer[1].

体外研究
(In Vitro)

TTK-IN-5 (Compound 19) (1 μM) 对苏氨酸酪氨酸激酶 (TTK) 具有强效且高度选择性的抑制活性,抑制率高达 98.99% (IC50 = 8.918 nM)[1]
TTK-IN-5 (5 μM, 12 小时) 与 TTK 形成强效相互作用并紧密结合[1]

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

体内研究
(In Vivo)

TTK-IN-5 (Compound 19) (7.5, 15 mg/kg, 静脉注射, 每周两次, 持续 21 天) 在 MDA-MB-231 异种移植小鼠模型中能显著抑制肿瘤生长,且毒性较低[1]
TTK-IN-5 (30 mg/kg, 口服, 每日一次, 持续 21 天) 在 A2780 异种移植小鼠模型中能抑制肿瘤生长[1]

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

Animal Model: MDA-MB-231 xenograft mouse model in female BALB/c nude mice (6-8 weeks)[1]
Dosage: 7.5, 15 mg/kg, Paclitaxel (HY-B0015) 10 mg/kg
Administration: Intravenous injection (i.v.), twice a week for 21 days
Result: Showed tumor growth inhibition (TGI) values of 49.3% and 66.0% at doses of 7.5 mg/kg and 15 mg/kg, respectively.
Markedly suppressed tumor growth (TGI = 75.0%), with no significant changes in animal body weights following combination treatment of Paclitaxel.
Inhibited tumor cell proliferation and markedly induced cell death when co-administrated with Paclitaxel.
Decreased phosphorylation of TTK in a dose dependent manner.
Increased Bax protein levels and suppressed Bcl-2 protein, explaining its apoptotic potency.
Animal Model: A2780 xenograft mouse model in female BALB/c nude mice (6-8 weeks)[1]
Dosage: 30 mg/kg
Administration: oral administration (p.o.), once daily for 21 days
Result: Effectively inhibited tumor growth, reaching the tumor growth inhibition (TGI) of 36.46%.
Significantly inhibited tumor volume.
Induced no significant changes in body weight.
分子量

533.53

Formula

C28H25F2N5O4

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
  • 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.

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产品名称:
TTK-IN-5
目录号:
HY-179430
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