Nelarabine

Catalog No.S1213 Synonyms: 506U78

Nelarabine  Chemical Structure

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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In DMSO USD 200 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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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.

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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.
Targets
DNA synthesis (PER-255 cells) [1] DNA synthesis (HSB2 cells) [1] DNA synthesis (ALL-SIL cells) [1] DNA synthesis (JURKAT cells) [1]
67 nM 0.44 μM 1.24 μM 2.15 μM
In vitro

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. [1] Nelarabine acts by inhibiting DNA synthesis and inducing apoptosis in susceptible cells. [2]Nelarabine demonstrated significant antineoplastic activity with acceptable toxicity. [3]

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. [4]

Protocol

Cell Research:sup>[1]
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  • Cell lines: HSB2, ALL-SIL, JURKAT and PER-255 cell lines
  • Concentrations: 0.125 μg/mL - 8 μg/mL
  • Incubation Time: 96 hours
  • Method: HSB2, ALL-SIL, JURKAT and PER-255 cell lines are tested for drug resistance using the MTT assay. Nelarabine are incubated over 4 days, with concentration tested in triplicate. The IC50 (drug concentration that inhibits cell growth by 50%) is used as the measure of drug resistance. Data represent the average of 2-6 experiments performed on separate occasions. In cases where 50% cytotoxicity is not achieved by even the highest dose in a particular experiment, the IC50 is recorded as double the highest concentration tested.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: Healthy adult male rhesus monkeys
  • Formulation: Control
  • Dosages: 35 mg/kg
  • Administration: Administered via i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 60 mg/mL (201.83 mM)
Water 3 mg/mL (10.09 mM)
Ethanol Insoluble
In vivo Add solvents individually and in order:
saline
3mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 297.27
Formula

C11H15N5O5

CAS No. 121032-29-9
Storage powder
Synonyms 506U78

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID