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.
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- Pureza : 99.87%
- No. CAS: 849550-67-0
- Fòrmula: C22H22ClF5N6O5
- Peso molecular:580.89
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Almacenamiento:
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Cevipabulin fumarate
More
Actividad biológica
Descripciòn
IC50 & Target
IC50: 18-40 nM (microtubule in human tumor cells)[1].
In Vitro
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.
In Vivo
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.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 849550-67-0
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Appearance Solid
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Peso molecular 580.89
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Fòrmula 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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Synonyms
TTI-237 fumarate
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
Solvente y solubilidad
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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 Related Classifications
HY-14949C Related Classifications
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