KPT-185
目录号 : GC14517
An inhibitor of XPO1/CRM1
Cas No.:1333151-73-7
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1,2]: | |
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Cell lines |
AML cell lines MV4-11, MOLM-13,OCI-AML3, Kasumi-1, KG1a,Thp-1; pancreatic cancer cells |
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Preparation method |
The solubility of this compound in DMSO is >17.8mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
IC50: 100 nM-500 nM, 24h |
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Applications |
Submicromolar concentrations of KPT-185 inhibited leukemia cell proliferation, with IC50 values ranging from 100nM to 500nM. KPT-185 induced cell-cycle arrest at G1 in MV4-11, OCI/AML3, and MOLM-13 cells at 24 hours. KPT-185 inhibited cell proliferation and induced apoptosis in primary AML blasts. KPT-185 treatment decreased c-KIT protein level in Kasumi-1 and OCI-AML3 cells. KPT-185 inhibited proliferation and promoted apoptosis of pancreatic cancer cells. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. |
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| Cas No. | 1333151-73-7 | SDF | |
| 化学名 | propan-2-yl (Z)-3-[3-[3-methoxy-5-(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]prop-2-enoate | ||
| Canonical SMILES | CC(C)OC(=O)C=CN1C=NC(=N1)C2=CC(=CC(=C2)OC)C(F)(F)F | ||
| 分子式 | C16H16F3N3O3 | 分子量 | 355.31 |
| 溶解度 | ≥ 17.8mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8144 mL | 14.0722 mL | 28.1444 mL |
| 5 mM | 0.5629 mL | 2.8144 mL | 5.6289 mL |
| 10 mM | 0.2814 mL | 1.4072 mL | 2.8144 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
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：取 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 saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet