MKI-1(Synonyms: MASTL Kinase Inhibitor-1)

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MKI-1 (Synonyms: MASTL Kinase Inhibitor-1) 纯度: 98.27%

MKI-1 是微管相关丝氨酸/苏氨酸样激酶 (MASTL) 的抑制剂，其IC50 为9.9 μM。MKI-1 通过激活乳腺癌中的PP2A 发挥抗肿瘤和放射增敏活性。

MKI-1(Synonyms: MASTL Kinase Inhibitor-1)

MKI-1 Chemical Structure

CAS No. : 1190277-80-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3300 In-stock
5 mg ￥3000 In-stock
10 mg ￥5000 In-stock
25 mg ￥9500 In-stock
50 mg ￥15500 In-stock
100 mg ￥23500 In-stock
200 mg   询价  
500 mg   询价  

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MKI-1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Breast Cancer Compound Library
  • Targeted Diversity Library

生物活性

MKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 of 9.9 μM, exerts antitumor and radiosensitizer activities through PP2A activation in breast cancer[1].

体外研究
(In Vitro)

MKI-1 (5-20 μM) inhibits the activity of MASTL in breast cancer cells[1].
MKI-1 (100 μM, 72 h) inhibits various oncogenic properties of breast cancer cells but showed much weaker effects on the viability of normal breast cells[1].
MKI-1 clearly reduces both serine 62-phosphorylation of c-Myc and total c-Myc, with a decrease in ENSA phosphorylation[1].
MKI-1 (20 μM, 16 h) reduces c-Myc stability through PP2A activation in MCF7 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MCF7 and T47D cells.
Concentration: 5-20 μM.
Incubation Time: 24 h.
Result: Inhibited the phosphorylation of ENSA in MCF7 and T47D cells.
Significantly inhibited the phosphorylation of ENSA in mitotic cells.

体内研究
(In Vivo)

MKI-1 (50 mg/kg, ip, twice a week) reduces tumor growth and enhances the radiosensitivity of BT549 xenograft model in response to 6 Gy irradiation compared with the control group, with no notable changes in body weight, suggesting the absence of gross toxicity in the treated mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Five-week-old female BALB/c nude mice (BT549 cells)[1].
Dosage: 50 mg/kg.
Administration: Twice per week by intraperitoneal (i.p.) injection.
Result: Reduced tumor growth.

分子量

302.33

Formula

C18H14N4O
CAS 号

1190277-80-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (826.91 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3076 mL 16.5382 mL 33.0764 mL
5 mM 0.6615 mL 3.3076 mL 6.6153 mL
10 mM 0.3308 mL 1.6538 mL 3.3076 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Ah-Young Kim, et al. MKI-1, a Novel Small-Molecule Inhibitor of MASTL, Exerts Antitumor and Radiosensitizer Activities Through PP2A Activation in Breast cancer. Front Oncol. 2020 Sep 29;10:571601.

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