Catalog No.S1213 Synonyms: 506U78
Molecular Weight(MW): 297.27
Nelarabine is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.
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b) Western blot analysis documenting cleavage of caspase-8, caspase-9, caspase-3, and PARP by nelarabine. Cells were treated with nelarabine (5 μM for JURKAT, P12-ICHIKAWA, and DND-41 cells, 2 μM MOLT-4 cells) for the indicated times, collected, and then lysed. Fifty micrograms of each lysate were electrophoresed on SDS-PAGE gels followed by transfer onto a nitrocellulose membrane. c) Nelarabine induces a decrease in the phosphorylation status of critical components of the PI3K/AKT/mTOR signaling pathway, as well as p-ERK (Thr202) levels in T-ALL sensitive cell lines. Western blot analysis documenting the reduction of p-AKT (Ser473), p-S6RP, p-GSK3β (Ser9), and p-ERK (Thr202). Antibody to β-actin served as a loading control. Molecular weights are indicated on the right
J Hematol Oncol, 2016, 9(1):114.. Nelarabine purchased from Selleck.
Purity & Quality Control
Choose Selective DNA/RNA Synthesis Inhibitors
|Description||Nelarabine is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.|
|Features||Nelarabine is rapidly converted into ara-G through demethoxylation by adenosine deaminase.|
The IC50 of Nelarabine is 25-fold and 113-fold higher than ARAC in T- and B-lineage, respectively. T-ALL cells are eightfold more sensitive to Nelarabine than B-lineage but there is considerable overlap. The efficacy of NEL in T-lineage and B-lineage cell lines is 25-fold and 113-fold less than ARAC, respectively.  Nelarabine acts by inhibiting DNA synthesis and inducing apoptosis in susceptible cells. Nelarabine demonstrated significant antineoplastic activity with acceptable toxicity. 
|In vivo||The Nelarabine plasma AUC is 2.82 mM minutes and the ara-G plasma AUC is 20 mM minutes. The terminal half-life of Nelarabine in plasma is 25 min, clearance is 42 mL/minutes/kg, and central volume of distribution is 1.1 L/kg. The terminal half-life of ara-G in plasma is 182 minutes and the central volume of distribution is 1.4 L/kg. In CSF the terminal half-life of Nelarabine is 77 minutes and of ara-G is 232 minutes. The AUCcsf:AUCplasma is 29 % for Nelarabine and 23 % for ara-G. Nelarabine and ara-G do not accumulate with daily infusions because of their relatively short half-lives. |
|In vitro||DMSO||60 mg/mL (201.83 mM)|
|Water||3 mg/mL (10.09 mM)|
|In vivo||Add solvents individually and in order:
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03020030||Not yet recruiting||Acute Lymphoblastic Leukemia, Pediatric||Dana-Farber Cancer Institute|Baxalta US Inc.||January 2017||Phase 3|
|NCT02881086||Recruiting||Acute Lymphoblastic Leukemia|Lymphoblastic Lymphoma||Johann Wolfgang Goethe University Hospital||August 2016||Phase 3|
|NCT02619630||Recruiting||T-cell Adult Acute Lymphoblastic Leukemia||Assistance Publique - Hôpitaux de Paris||December 2015||Phase 2|
|NCT02518750||Recruiting||Acute Lymphoblastic Leukemia|Lymphoma, Non-Hodgkins|Leukemia, T-Cell|Leukemia, B-Cell||St. Jude Childrens Research Hospital|Novartis Pharmaceuticals|Spectrum Pharmaceuticals, Inc||December 2015||Phase 2|
|NCT01094860||Active, not recruiting||Leukemia||M.D. Anderson Cancer Center|GlaxoSmithKline||June 2010||Phase 1|
|NCT00981799||Terminated||Relapsed T-Cell Acute Lymphoblastic Leukemia|Relapsed T-Cell Lymphoblastic Lymphoma||Therapeutic Advances in Childhood Leukemia Consortium|GlaxoSmithKline|Novartis||June 2010||Phase 1|Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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