Troxacitabine
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Troxacitabine is nucleoside analog with potent anticancer activity.
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- Pureza: 99.95%
- No. CAS: 145918-75-8
- Fòrmula: C8H11N3O4
- Peso molecular:213.19
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Actividad biológica
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.68 μM
Compound: 5
|
Cytotoxicity against A549 cells after 72 hrs by SRB assay
Cytotoxicity against A549 cells after 72 hrs by SRB assay
|
[PMID: 17419604] |
| CCRF-CEM | IC50 |
>1 μM
Compound: beta-L-cytosine
|
Compound was evaluated for cytotoxicity by inhibition of mitochondrial DNA synthesis
Compound was evaluated for cytotoxicity by inhibition of mitochondrial DNA synthesis
|
10.1016/0960-894X(95)00343-R |
| CCRF-CEM | IC50 |
0.056 μM
Compound: beta-L-cytosine
|
Cytotoxicity in H1 CEM cells
Cytotoxicity in H1 CEM cells
|
10.1016/0960-894X(95)00343-R |
| Hepatoma cell line | EC50 |
0.0005 μM
Compound: beta-L-cytosine
|
Antiviral activity against hepatitis B virus in human hepatoma cell line (2.2.15 cells)
Antiviral activity against hepatitis B virus in human hepatoma cell line (2.2.15 cells)
|
10.1016/0960-894X(95)00343-R |
| Hepatoma cell line | EC50 |
0.5 nM
Compound: beta-L-cytosine
|
Antiviral activity against hepatitis B virus in human hepatoma cell line (2.2.15 cells)
Antiviral activity against hepatitis B virus in human hepatoma cell line (2.2.15 cells)
|
10.1016/0960-894X(95)00343-R |
| SW1573 | IC50 |
2.3 μM
Compound: 5
|
Cytotoxicity against SW1573 cells after 72 hrs by SRB assay
Cytotoxicity against SW1573 cells after 72 hrs by SRB assay
|
[PMID: 17419604] |
| Vero | IC50 |
0.1 μM
Compound: 25
|
Cytotoxic effect against vero cells.
Cytotoxic effect against vero cells.
|
[PMID: 8496934] |
Troxacitabine has shown cutotoxicity in cancer cell lines of hepatocellular (HepG2), prostate (PC3, DUI45), non-small cell lung (NCI-H460, NCr-322M) colon (HT29), renal (CAK-l, A498, RXF-393, SNI2-C) and pancreatic origin (Pnac-Ol, MiaPa Ca) with IC50s range from 15-35 μM[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 |
Chemical Information
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No. CAS 145918-75-8
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Appearance Solid
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Peso molecular 213.19
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Fòrmula C8H11N3O4
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Color White to off-white
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SMILES
NC1=NC(N(C=C1)[C@@H]2CO[C@H](CO)O2)=O
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Synonyms
BCH 4556; L-OddC; SPD 758
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 20 mg/mL (93.81 mM; Need ultrasonic; 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocolo
Mice[3]
Troxacitabine is administered i.v. to the animals at doses of 10 and 25 mg/kg on a daily 3 5 regimen. Gemcitabine is used as a positive control. The end points for the study included tumor growth inhibition (TGI), final weight, and the number of partial and complete tumor responses in the animals[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (276 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Gourdeau H, et al. Antitumor activity of troxacitabine (Troxatyl) against anthracycline-resistant human xenografts. Cancer Chemother Pharmacol. 2002 Dec;50(6):490-6. [Content Brief]
[2]. Kadhim SA, et al. Potent antitumor activity of a novel nucleoside analogue, BCH-4556 (beta-L-dioxolane-cytidine), in human renal cell carcinoma xenograft tumor models. Cancer Res. 1997 Nov 1;57(21):4803-10. [Content Brief]
[3]. Weitman S, et al. The new dioxolane, (-)-2'-deoxy-3'-oxacytidine (BCH-4556, troxacitabine), has activity againstpancreatic human tumor xenografts. Clin Cancer Res. 2000 Apr;6(4):1574-8. [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 (protect from light). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.6907 mL | 23.4533 mL | 46.9065 mL | 117.2663 mL |
| 5 mM | 0.9381 mL | 4.6907 mL | 9.3813 mL | 23.4533 mL | |
| 10 mM | 0.4691 mL | 2.3453 mL | 4.6907 mL | 11.7266 mL | |
| 15 mM | 0.3127 mL | 1.5636 mL | 3.1271 mL | 7.8178 mL | |
| 20 mM | 0.2345 mL | 1.1727 mL | 2.3453 mL | 5.8633 mL | |
| 25 mM | 0.1876 mL | 0.9381 mL | 1.8763 mL | 4.6907 mL | |
| 30 mM | 0.1564 mL | 0.7818 mL | 1.5636 mL | 3.9089 mL | |
| 40 mM | 0.1173 mL | 0.5863 mL | 1.1727 mL | 2.9317 mL | |
| 50 mM | 0.0938 mL | 0.4691 mL | 0.9381 mL | 2.3453 mL | |
| 60 mM | 0.0782 mL | 0.3909 mL | 0.7818 mL | 1.9544 mL | |
| 80 mM | 0.0586 mL | 0.2932 mL | 0.5863 mL | 1.4658 mL |