Fazarabine
Fazarabine (Kymarabine; Ara-AC; NSC 281272) is an orally active, blood-brain barrier permeable DNA polymerase inhibitor and antitumor agent. Fazarabine interferes with DNA synthesis via intracellular activation into a triphosphate nucleotide that directly incorporates into DNA, inducing cytotoxicity, myelosuppression, as well as moderate nausea and vomiting. Fazarabine is resistant to deamination by cytidine-deoxycytidine deaminase and undergoes spontaneous aqueous degradation. Fazarabine exerts time-dependent, broad-spectrum activity against leukemia and solid tumors. Fazarabine can be used in research related to refractory malignancies, acute leukemia, and blast-phase chronic myeloid leukemia.
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- CAS. Nr.: 65886-71-7
- Formel: C8H12N4O5
- Molecular Weight:244.20
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
DNA Polymerases |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLT-4 | IC50 |
0.1 μM
|
Inhibition of clonogenic survival against human Molt-4 T-lymphoblastic leukemia cells in a 24 h in vitro clonogenic survival assay.
Inhibition of clonogenic survival against human Molt-4 T-lymphoblastic leukemia cells in a 24 h in vitro clonogenic survival assay.
|
2475244 |
In Vitro
Fazarabine exhibits broad-spectrum antitumor activity against the P388 and L1210 cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 65886-71-7
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Molecular Weight 244.20
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Formel C8H12N4O5
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SMILES
NC(N=CN1[C@H]2[C@@H](O)[C@H](O)[C@@H](CO)O2)=NC1=O
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Synonyms
Kymarabine; Ara-AC; NSC 281272
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Keywords
- Fazarabine
- 65886-71-7
- Kymarabine
- Ara-AC
- NSC 281272
- NSC281272
- NSC 281272
- NSC-281272
- DNA/RNA Synthesis
- L1210 cell lines
- cytidine-deoxycytidine deaminase
- P388 cell lines
- DNA polymerase
- Molt-4 human T-lymphoblastic leukemia cells
- chronic myelogenous leukemia
- acute leukemia
- cerebrospinal fluid
- murine L1210 leukemias
- blood-brain barrier
- Inhibitor
- inhibitor
- inhibit