Crolibulin
Based on 1 publication(s) in Google Scholar
Crolibulin (EPC2407) is a tubulin polymerization inhibitor, with potent apoptosis induction and cell growth inhibition. Crolibulin has anti-tumor activity. Crolibulin also has cardiovascular toxicity and neurotoxicity.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.96%
- CAS 番号: 1000852-17-4
- 分子式: C18H17BrN4O3
- 分子量:417.26
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 Crolibulin
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生物活性
Tubulin polymerization[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.39 μM
Compound: Crolibulin
|
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
|
[PMID: 29407949] |
| HT-29 | IC50 |
0.55 μM
Compound: Crolibulin
|
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
|
[PMID: 29407949] |
| MKN-45 | IC50 |
0.17 μM
Compound: Crolibulin
|
Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay
Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay
|
[PMID: 29407949] |
| NCI-H460 | IC50 |
0.03 μM
Compound: Crolibulin
|
Antiproliferative activity against human H460 cells after 72 hrs by MTT assay
Antiproliferative activity against human H460 cells after 72 hrs by MTT assay
|
[PMID: 29407949] |
Crolibulin shows significant cytotoxic activity against HT-29 cells, with an IC50 of 0.52 μM[2].
Crolibulin is active against various experimental tumors and exhibit potent inhibition of mitosis at the G2/M stage[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1000852-17-4
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性状 Solid
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分子量 417.26
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分子式 C18H17BrN4O3
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Color Light yellow to yellow
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SMILES
N#CC1=C(N)OC2=C(N)C(N)=CC=C2[C@H]1C3=CC(OC)=C(OC)C(Br)=C3
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別名
EPC2407
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Biochem Biophys Res Commun
Molecular mechanism of crolibulin in complex with tubulin provides a rationale for drug design. [Abstract]2019 Apr 2;511(2):381-386. PMID: 30803758
溶剤 & 溶解度
DMSO : 125 mg/mL (299.57 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kalmuk J, et al. Multimodal imaging guided preclinical trials of vascular targeting in prostate cancer. Oncotarget. 2015 Sep 15;6(27):24376-92. [Content Brief]
[2]. Zhai X, et al. Discovery and Optimization of Novel 5-Indolyl-7-arylimidazo[1,2-a]pyridine-8-carbonitrile Derivatives as Potent Antitubulin Agents Targeting Colchicine-binding Site. Sci Rep. 2017 Feb 27;7:43398. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3966 mL | 11.9829 mL | 23.9659 mL | 59.9147 mL |
| 5 mM | 0.4793 mL | 2.3966 mL | 4.7932 mL | 11.9829 mL | |
| 10 mM | 0.2397 mL | 1.1983 mL | 2.3966 mL | 5.9915 mL | |
| 15 mM | 0.1598 mL | 0.7989 mL | 1.5977 mL | 3.9943 mL | |
| 20 mM | 0.1198 mL | 0.5991 mL | 1.1983 mL | 2.9957 mL | |
| 25 mM | 0.0959 mL | 0.4793 mL | 0.9586 mL | 2.3966 mL | |
| 30 mM | 0.0799 mL | 0.3994 mL | 0.7989 mL | 1.9972 mL | |
| 40 mM | 0.0599 mL | 0.2996 mL | 0.5991 mL | 1.4979 mL | |
| 50 mM | 0.0479 mL | 0.2397 mL | 0.4793 mL | 1.1983 mL | |
| 60 mM | 0.0399 mL | 0.1997 mL | 0.3994 mL | 0.9986 mL | |
| 80 mM | 0.0300 mL | 0.1498 mL | 0.2996 mL | 0.7489 mL | |
| 100 mM | 0.0240 mL | 0.1198 mL | 0.2397 mL | 0.5991 mL |