Thiarabine
Based on 1 Customer Validation
Thiarabine (OSI-7836) is an orally active cytotoxic antitumor agent that acts as a deoxycytidine kinase substrate and a DNA chain terminator. Thiarabine is metabolized to form its major active metabolite T-araCTP, which potently inhibits DNA synthesis and exhibits a long retention time in tumor cells. Thiarabine is widely applicable to research related to leukemia, lymphoma, hematologic malignancies, acute myeloid leukemia, and advanced solid malignancies.
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- Pureza: 99.66%
- No. CAS: 26599-17-7
- Fòrmula: C9H13N3O4S
- Peso molecular:259.28
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HFF | CC50 |
>100 μM
Compound: 5
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Cytotoxicity against HFF after 3 days by MTS assay
Cytotoxicity against HFF after 3 days by MTS assay
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[PMID: 19770274] |
| HFF | CC50 |
>88 μM
Compound: 10
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Cytotoxicity against HFF after 7 days by neutral red uptake assay
Cytotoxicity against HFF after 7 days by neutral red uptake assay
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[PMID: 19029322] |
| HFF | IC50 |
1 μM
Compound: 10
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Antiproliferative activity against HFF after 3 days by coulter counter assay
Antiproliferative activity against HFF after 3 days by coulter counter assay
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[PMID: 19029322] |
| HFF | IC50 |
1 μM
Compound: 5
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Antiproliferative activity against HFF after 3 days by Coulter counting analysis
Antiproliferative activity against HFF after 3 days by Coulter counting analysis
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[PMID: 19770274] |
| PANC-1 | CC50 |
0.59 μM
Compound: 55
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Cytotoxicity against human PANC-1 cells
Cytotoxicity against human PANC-1 cells
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[PMID: 38056297] |
| U-87MG ATCC | CC50 |
0.59 μM
Compound: 55
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Cytotoxicity against human U-87 MG cells
Cytotoxicity against human U-87 MG cells
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[PMID: 38056297] |
In Vitro
Thiarabine (1-10 μM) potently inhibits the growth of a panel of human tumor cell lines with IC50 values of 1 to 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Thiarabine (22.5-90 mg/kg/dose; i.p.; daily; 9 consecutive days, days 1-9) is fully ineffective against thiarabine-resistant P388/T-araC leukemia in CD2F1 mice[1].
Thiarabine (100 mg/kg/dose; i.p.; single dose) is converted to its active metabolite T-araCTP at comparable levels in both thiarabine-sensitive P388/0 and thiarabine-resistant P388/T-araC leukemia cells in CD2F1 mice following a 100 mg/kg i.p. dose[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD2F1 Mice (female, implanted intraperitoneally with 10^6 parental P388/0 leukemia cells)[1]
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Dosage:45 mg/kg/dose; 90 mg/kg/dose
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Administration:i.p.; daily; 9 consecutive days (days 1-9)
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Result:Produced a median increase in lifespan (ILS) of +136% in passage 0 parental P388/0-bearing mice, with a median treated lifespan of 26.0 days versus 11.0 days in untreated controls.
Produced median ILS values ranging from +163% to +220% and net log10 cell kill values ranging from +6.3 to >6.9 units (approximately 1,000,000-fold reduction in tumor burden) across four studies in parental P388/0-bearing mice; 1/6 mice were long-term (60-day) survivors in two of these studies.
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Animal Model:CD2F1 Mice (female, implanted intraperitoneally with 10^6 thiarabine-resistant P388/T-araC leukemia cells)[1]
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Dosage:22.5 mg/kg/dose; 45 mg/kg/dose; 90 mg/kg/dose
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Administration:i.p.; daily; 9 consecutive days (days 1-9)
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Result:Produced median ILS values ranging from +4% to +13% across passage 8, 21, and selection studies in P388/T-araC-bearing mice, with median treated lifespans only marginally longer than untreated controls.
Produced median ILS values ranging from 0% to +9% and net log10 cell kill values of -1.8 to -1.9 units (almost 100-fold leukemia growth during treatment) across four studies in P388/T-araC-bearing mice; no long-term (60-day) survivors were observed.
Produced a median ILS of +8% in passage 8 P388/T-araC-bearing mice.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 26599-17-7
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Appearance Solid
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Peso molecular 259.28
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Fòrmula C9H13N3O4S
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Color White to off-white
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SMILES
O[C@H]1[C@H](O)[C@@H](CO)S[C@H]1N2C=CC(N)=NC2=O
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Synonyms
OSI-7836
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (385.68 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. 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. 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)
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Waud WR, et al.. Isolation and characterization of a murine P388 leukemia line resistant to thiarabine. Nucleosides, nucleotides & nucleic acids. 2012;31(1):14-27. [Content Brief]
[2]. Parker WB, et al.. Thiarabine, 1-(4-Thio-β-D-arabinofuranosyl)cytosine. A Deoxycytidine Analog With Excellent Anticancer Activity. Current medicinal chemistry. 2015;22(34):3881-96. [Content Brief]
[3]. Jordheim LP, et al.. Advances in the development of nucleoside and nucleotide analogues for cancer and viral diseases. Nature reviews. Drug discovery. 2013 Jun;12(6):447-64. [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. 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 | 3.8568 mL | 19.2842 mL | 38.5683 mL | 96.4209 mL |
| 5 mM | 0.7714 mL | 3.8568 mL | 7.7137 mL | 19.2842 mL | |
| 10 mM | 0.3857 mL | 1.9284 mL | 3.8568 mL | 9.6421 mL | |
| 15 mM | 0.2571 mL | 1.2856 mL | 2.5712 mL | 6.4281 mL | |
| 20 mM | 0.1928 mL | 0.9642 mL | 1.9284 mL | 4.8210 mL | |
| 25 mM | 0.1543 mL | 0.7714 mL | 1.5427 mL | 3.8568 mL | |
| 30 mM | 0.1286 mL | 0.6428 mL | 1.2856 mL | 3.2140 mL | |
| 40 mM | 0.0964 mL | 0.4821 mL | 0.9642 mL | 2.4105 mL | |
| 50 mM | 0.0771 mL | 0.3857 mL | 0.7714 mL | 1.9284 mL | |
| 60 mM | 0.0643 mL | 0.3214 mL | 0.6428 mL | 1.6070 mL | |
| 80 mM | 0.0482 mL | 0.2411 mL | 0.4821 mL | 1.2053 mL | |
| 100 mM | 0.0386 mL | 0.1928 mL | 0.3857 mL | 0.9642 mL |
Thiarabine Related Classifications
HY-16496 Related Classifications
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