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OTSSP167

现货
Catalog No.
B1321
MELK抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,500.00
现货
10mg
¥ 2,400.00
现货
50mg
¥ 7,500.00
Ship with 10-15 days
200mg
¥ 22,990.00
Ship with 10-15 days

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Background

OTSSP167 is an inhibitor of maternal embryonic leucine zipper kinase (MELK) with IC50 value of 0.41nM [1].

MELK is a member of the AMPK serine/threonine kinase family and is involved in the mammalian embryonic development. It plays roles in cancer cell growth and formation or maintenance of cancer stem cells. OTSSP167 is a small-molecule inhibitor and can inhibit MELK’s activity effectively and selectively. OTSSP167 inhibits cell proliferation of a variety of cancer cell lines including A549, T47D, DU4475 and 22Rv1. The IC50 values are 6.7nM, 4.3nM, 2.3nM and 6nM, respectively. In mice bearing MDA-MB-231 xenograft, administration of OTSSP167 inhibits 70% tumor growth at dose of 20 mg/kg. Besides that, OTSSP167 is also found to have effects on PSMA1 and DBNL which are the novel substrates of MELK. It inhibits the phosphorylation of PSMA1 and DBNL causes the subsequent suppression of mammosphere formation [1].

References:
[1] Chung S, Suzuki H, Miyamoto T, et al. Development of an orally-administrative MELK-targeting inhibitor that suppresses the growth of various types of human cancer. Oncotarget, 2012, 3(12): 1629.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt487.42
Cas No.1431697-89-0
FormulaC25H28Cl2N4O2
Solubility<0.97mg/mL in DMSO
Chemical Name4-[7-acetyl-8-[[4-[(dimethylamino)methyl]cyclohexyl]amino]-1H-1,5-naphthyridin-2-ylidene]-2,6-dichlorocyclohexa-2,5-dien-1-one
SDFDownload SDF
Canonical SMILESCC(=O)C1=CN=C2C=CC(=C3C=C(C(=O)C(=C3)Cl)Cl)NC2=C1NC4CCC(CC4)CN(C)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

A549、T47D、DU4475和22Rv1肿瘤细胞系

溶解方法

在DMSO中溶解度有限。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

30 μM,37 °C

应用

OTSSP167抑制A549(肺)、T47D(乳腺)、DU4475(乳腺)和22Rv1(前列腺)癌细胞,IC50值分别为6.7、4.3、2.3和6.0 nM。OTSSP167抑制PSMA1和DBNL的磷酸化。OTSSP167通过抑制PSMA1磷酸化来抑制乳腺癌细胞的乳房球形成。

动物实验 [1]:

动物模型

携带MDA-MB-231异种移植物的小鼠,携带A549肺癌异种移植物的小鼠

给药剂量

静脉注射,20 mg/kg,每两天一次;口服,10 mg/kg,每日一次

应用

在携带MDA-MB-231异种移植物的小鼠中,每两天静脉内给药OTSSP167 20 mg/kg造成73%的肿瘤生长抑制(TGI)。口服10 mg/kg,每天一次,TGI为72%。在携带A549(肺癌)异种移植物的小鼠中,通过静脉内给药每天一次,每次1 mg/kg、 5 mg/kg和10 mg/kg的TGI分别为51、91和108%,口服5和20 mg/kg,每天一次,TGI分别为95和124%。在DU145(前列腺癌)和MIAPaCa-2(胰腺癌)异种移植模型中,每天口服10 mg/kg OTSSP167,TGI分别为106和87%。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Chung S, Suzuki H, Miyamoto T, et al. Development of an orally-administrative MELK-targeting inhibitor that suppresses the growth of various types of human cancer[J]. Oncotarget, 2012, 3(12): 1629.

生物活性

Description OTSSP167是母系胚胎亮氨酸拉链蛋白激酶(MELK)的抑制剂,其IC50值为0.41 nM.
靶点 MELK          
IC50 0.41nM          

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