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MKI-1 (Synonyms:MASTL Kinase Inhibitor-1)
目录号 : KM6244 CAS No. : 1190277-80-5 纯度 : 98%

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。

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5mg
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10mg
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25mg
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50mg
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100mg
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200mg 询价 In-stock
500mg 询价 In-stock

Other Forms of Rapamycin:

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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.

体外研究

MKI-1 (5-20 μM) inhibits the activity of MASTL in breast cancer cells.
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.
MKI-1 clearly reduces both serine 62-phosphorylation of c-Myc and total c-Myc, with a decrease in ENSA phosphorylation.
MKI-1 (20 μM, 16 h) reduces c-Myc stability through PP2A activation in MCF7 cells.

Western Blot Analysis

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

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.

Animal Model: Five-week-old female BALB/c nude mice (BT549 cells).
Dosage: 50 mg/kg.
Administration: Twice per week by intraperitoneal (i.p.) injection.
Result: Reduced tumor growth.
分子式
C18H14N4O
分子量
302.33
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。

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工作液浓度 mg/ml;

DMSO母液配制方法 mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,

体内配方配制方法μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

配置后的溶液总体积

1. 首先保证母液是澄清的;
           2. 一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。