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Submit ReviewClofarabine is a deoxycytidine kinase (dCK) substrate. Phosphorylated to form clofarabine triphosphate, which competes with dATP for DNA polymerase-α and -ε and potently inhibits ribonucleotide reductase (IC50 = 65 nM). Induces apoptosis by directly altering mitochondrial transmembrane potential. Demonstrates growth inhibition and cytotoxic activity in a variety of leukemias and solid tumors.
Clofarabine is also offered as part of the Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 303.68 |
公式 | C10H11ClFN5O3 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 123318-82-1 |
PubChem ID | 119182 |
InChI Key | WDDPHFBMKLOVOX-AYQXTPAHSA-N |
Smiles | O[C@@H]1[C@@H](CO)O[C@@H](N(C=N3)C2=C3C(N)=NC(Cl)=N2)[C@H]1F |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Parker et al (1991) Effects of 2-chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl) adenine on K562 cellular metabolism and the inhibition of human ribonucleotide reductase and DNA polymerases by its 5'-triphosphate. Cancer Res. 51 2386 PMID: 1707752
Bonate et al (2006) Discovery and development of clofarabine: a nucleoside analogue for treating cancer. Nat.Rev.Drug Discov. 5 855 PMID: 17016426
Carson et al (1992) Oral antilymphocyte activity and induction of apoptosis by 2-chloro-2'-arabino-fluoro-2'-deoxyadenosine. Proc.Natl.Acad.Sci.USA 89 2970
关键词: Clofarabine, Clofarabine supplier, Deoxycytidine, kinases, dCK, Enzyme, Substrates, activators, antimetabolites, chemotherapeutics, /, Activators, Other, Kinases, 2600, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Clofarabine 的部分引用包括:
Xie et al (2012) Valproic acid synergistically enhances the cytotoxicity of clofar. in pediatric acute myeloid leukemia cells. Pediatr Blood Cancer 59 1245 PMID: 22488775
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