Cevipabulin fumarate
Based on 2 publication(s) in Google Scholar
Cevipabulin fumarate (TTI-237 fumarate) is an oral, microtubule-active, antitumor compound and inhibits the binding of [3H]NSC 49842 to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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 : 99.87%
- CAS 番号: 849550-67-0
- 分子式: C22H22ClF5N6O5
- 分子量:580.89
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Cevipabulin fumarate
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生物活性
製品説明
IC50 & Target
IC50: 18-40 nM (microtubule in human tumor cells)[1].
体外実験
Cevipabulin (0-50 nM, 72 hours) shows good activity (between 18 and 40 nM IC50 values) on cell lines from ovarian, breast, prostate, and cervical tumors[1].
Flow cytometry experiments reveal that, Cevipabulin (TTI-237) at low concentrations (20-40 nM) produces sub-G1 nuclei and, at concentrations above 50 nM, it causes a strong G2-M block[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human cancer cell lines (SK-OV-3, MDA-MB-435, MDA-MB-468, LnCaP, and Hela cells).
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Concentration:0-50 nM
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Incubation Time:72 hours
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Result:The IC50 values are 24±8 nM, 21±4 nM, 18±6 nM, 22±7 nM and 40 nM in SK-OV-3, MDA-MB-435, MDA-MB-468, LnCaP and Hela cells.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic nu/nu female mice implanted s.c. in the flank with 1×107 LoVo human colon adenocarcinoma cells[1].
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Dosage:5, 10, 15, and 20 mg/kg
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Administration:I.V. injection every 4 days for 4 cycles.
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Result:The compound showed dose-dependent effects, with good antitumor activity at 20 and 15 mg/kg.
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Animal Model:Athymic nu/nu female mice implanted s.c. in the flank with 1×106 U87-MG human glioblastoma cells[1].
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Dosage:25 mg/kg.
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Administration:P.O. or I.V. on days 0, 7, 14.
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Result:The compound was active by p.o. or i.v. administration against human tumor xenografts.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 849550-67-0
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性状 Solid
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分子量 580.89
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分子式 C22H22ClF5N6O5
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Color White to off-white
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SMILES
C[C@@H](C(F)(F)F)NC1=C(C2=C(F)C=C(OCCCNC)C=C2F)C(Cl)=NC3=NC=NN13.O=C(O)/C=C/C(O)=O
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別名
TTI-237 fumarate
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Biochem Biophys Res Commun
2019 Aug 27;516(3):760-764. PMID: 31253401
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (86.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1.43 mg/mL (2.46 mM; ultrasonic and warming and heat to 60°C)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (279 KB)
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SDS (252 KB)
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- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Beyer CF, et al. TTI-237: a novel microtubule-active compound with in vivo antitumor activity. Cancer Res. 2008 Apr 1;68(7):2292-300. [Content Brief]
[2]. Beyer CF, et al. The microtubule-active antitumor compound TTI-237 has both DB01229-like and Leurocristine-like properties. Cancer Chemother Pharmacol. 2009 Sep;64(4):681-9. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.7215 mL | 8.6075 mL | 17.2150 mL | 43.0374 mL |
| DMSO | 5 mM | 0.3443 mL | 1.7215 mL | 3.4430 mL | 8.6075 mL |
| 10 mM | 0.1721 mL | 0.8607 mL | 1.7215 mL | 4.3037 mL | |
| 15 mM | 0.1148 mL | 0.5738 mL | 1.1477 mL | 2.8692 mL | |
| 20 mM | 0.0861 mL | 0.4304 mL | 0.8607 mL | 2.1519 mL | |
| 25 mM | 0.0689 mL | 0.3443 mL | 0.6886 mL | 1.7215 mL | |
| 30 mM | 0.0574 mL | 0.2869 mL | 0.5738 mL | 1.4346 mL | |
| 40 mM | 0.0430 mL | 0.2152 mL | 0.4304 mL | 1.0759 mL | |
| 50 mM | 0.0344 mL | 0.1721 mL | 0.3443 mL | 0.8607 mL | |
| 60 mM | 0.0287 mL | 0.1435 mL | 0.2869 mL | 0.7173 mL | |
| 80 mM | 0.0215 mL | 0.1076 mL | 0.2152 mL | 0.5380 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Cevipabulin fumarate 関連分類
HY-14949C 関連分類
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