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.
For research use only. We do not sell to patients.
- CAS No.: 65886-71-7
- Formula: C8H12N4O5
- Molecular Weight:244.20
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All DNA/RNA Synthesis Isoforms
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Biological Activity
Description
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
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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.
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2475244 |
In Vitro
Fazarabine (0.1-1 μM; 24 h) reduces the clonogenic survival rate of the human T-lymphoblastic leukemia cell line Molt-4: after 24 h of exposure, the inhibition rate reaches 50% at 0.1 μM and 98% at 1 μM[1].
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 No. 65886-71-7
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Molecular Weight 244.20
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Fazarabine Related Classifications
HY-123113 Related Classifications
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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