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KPT-185

现货
Catalog No.
B1462
可逆的CRM1选择性抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 600.00
现货
10mg
¥ 680.00
现货
50mg
¥ 1,890.00
Ship with 10-15 days

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Background

KPT-185 is a selective and irreversible inhibitor of chromosome maintenance protein 1 (CRM1) with IC50 values of 100-500nM [1].

CRM1 is an important nuclear protein export receptor. Blocking CRM1-mediated nuclear export can result in the suppression of tumors. As an inhibitor of CRM1, KPT-185 binds CRM1within the Cys528 site and prevents CRM1from interacting with tumor-suppressor proteins. In the in vitro studies on AML cell lines, KPT-185 inhibits proliferation of a variety of leukemia cells with IC50 values ranging from 100nM to 500nM. It induces cell-cycle arrest at G1 and induces apoptosis. KPT-185 also strongly affects cell colony formation. In addition, the inhibition of CRM1 caused by KPT-185 induces differentiation of AML blast. Besides that, KPT-185 is also found to inhibit proliferation and induce apoptosis of pancreatic cancer cells including Colo-357, HPAC and BxPC-3 [1, 2].

References:
[1] Ranganathan P, Yu X, Na C, et al. Preclinical activity of a novel CRM1 inhibitor in acute myeloid leukemia. Blood, 2012, 120(9): 1765-1773.
[2] Azmi A S, Aboukameel A, Bao B, et al. Selective inhibitors of nuclear export block pancreatic cancer cell proliferation and reduce tumor growth in mice. Gastroenterology, 2013, 144(2): 447-456.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt355.31
Cas No.1333151-73-7
FormulaC16H16F3N3O3
Solubility≥17.8mg/mL in DMSO
Chemical Namepropan-2-yl (Z)-3-[3-[3-methoxy-5-(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]prop-2-enoate
SDFDownload SDF
Canonical SMILESCC(C)OC(=O)C=CN1C=NC(=N1)C2=CC(=CC(=C2)OC)C(F)(F)F
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 [1,2]:

细胞系

AML细胞系MV4-11、MOLM-13、OCI-AML3、Kasumi-1、KG1a、Thp-1;胰腺癌细胞。

溶解方法

该化合物在DMSO中的溶解度大于17.8 mg/mL。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

IC50: 100nM-500nM, 24h

应用

亚微摩尔浓度的KPT-185抑制白血病细胞增殖,IC50值范围为100 nM至500 nM。 在MV4-11、OCI/AML3和MOLM-13细胞中,KPT-185在24小时诱导细胞周期停滞。KPT-185抑制细胞增殖并诱导原代AML细胞凋亡。KPT-185处理降低了Kasumi-1和OCI-AML3细胞中的c-KIT蛋白水平。KPT-185抑制增殖,促进胰腺癌细胞凋亡。

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]. Ranganathan P, Yu X, Na C, et al. Preclinical activity of a novel CRM1 inhibitor in acute myeloid leukemia[J]. Blood, 2012, 120(9): 1765-1773.

[2]. Azmi A S, Aboukameel A, Bao B, et al. Selective inhibitors of nuclear export block pancreatic cancer cell proliferation and reduce tumor growth in mice[J]. Gastroenterology, 2013, 144(2): 447-456.

生物活性

Description KPT-185是一种CRM1的选择性抑制剂.
靶点 CRM1          
IC50            

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