MKI-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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, 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.

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.

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.

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1190277-80-5

302.33

C18H14N4O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (826.91 mM; 超声助溶 )

O=C(Nc1nc2ccccc2[nH]1)c1cccc(c1)-n1cccc1

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(-20℃)

With Ice Pack

≥ 2 years