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Chemical Structure| 121032-29-9 Chemical Structure| 121032-29-9

Structure of Nelarabine
CAS No.: 121032-29-9

Chemical Structure| 121032-29-9

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Nelarabine is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.

Synonyms: 506U78; GW 506U78; NS-686673

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Product Details of Nelarabine

CAS No. :121032-29-9
Formula : C11H15N5O5
M.W : 297.27
SMILES Code : O[C@@H]1[C@H](N2C=NC3=C(OC)N=C(N)N=C23)O[C@H](CO)[C@H]1O
Synonyms :
506U78; GW 506U78; NS-686673
MDL No. :MFCD00871078
InChI Key :IXOXBSCIXZEQEQ-UHTZMRCNSA-N
Pubchem ID :3011155

Safety of Nelarabine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Nelarabine

DNA

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
U937 3 μM 48 hours Evaluation of antiproliferative activity of Nelarabine on U937 cells, with an IC50 of 3 μM. PMC10094600
PEER cells 10 μM 48 hours Evaluate the effects of Nelarabine on resistant T-ALL cell lines. Results showed that Nelarabine caused hyperactivation of AKT and ERK1/2 signaling pathways and increased Bcl2 protein expression. PMC5075755
MOLT-16 cells 10 μM 48 hours Evaluate the effects of Nelarabine on resistant T-ALL cell lines. Results showed that Nelarabine caused hyperactivation of AKT and ERK1/2 signaling pathways and increased Bcl2 protein expression. PMC5075755
ALL-SIL cells 10 μM 48 hours Evaluate the effects of Nelarabine on resistant T-ALL cell lines. Results showed that Nelarabine caused hyperactivation of AKT and ERK1/2 signaling pathways and increased Bcl2 protein expression. PMC5075755
LOUCY cells 10 μM 48 hours Evaluate the effects of Nelarabine on resistant T-ALL cell lines. Results showed that Nelarabine caused hyperactivation of AKT and ERK1/2 signaling pathways and increased Bcl2 protein expression. PMC5075755
DND41 cells 5 μM 48 hours Evaluate the cytotoxicity and apoptosis-inducing effects of Nelarabine on T-ALL cell lines. Results showed that Nelarabine significantly increased the proportion of apoptotic cells and downregulated PI3K/AKT/mTOR and MEK/ERK1/2 signaling pathways. PMC5075755
P12-ICHIKAWA cells 5 μM 48 hours Evaluate the cytotoxicity and apoptosis-inducing effects of Nelarabine on T-ALL cell lines. Results showed that Nelarabine significantly increased the proportion of apoptotic cells and downregulated PI3K/AKT/mTOR and MEK/ERK1/2 signaling pathways. PMC5075755
JURKAT cells 5 μM 48 hours Evaluate the cytotoxicity and apoptosis-inducing effects of Nelarabine on T-ALL cell lines. Results showed that Nelarabine significantly increased the proportion of apoptotic cells and downregulated PI3K/AKT/mTOR and MEK/ERK1/2 signaling pathways. PMC5075755
MOLT-4 cells 2 μM 48 hours Evaluate the cytotoxicity and apoptosis-inducing effects of Nelarabine on T-ALL cell lines. Results showed that Nelarabine significantly increased the proportion of apoptotic cells and downregulated PI3K/AKT/mTOR and MEK/ERK1/2 signaling pathways. PMC5075755
T-ALL cells <450 nM (IC50) 72 hours Evaluate the antiproliferative activity of EdC against T-ALL cells, showing IC50 values below 450 nM for all tested cell lines PMC11286238

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice Mouse xenograft model of acute T-lymphoblastic leukemia Tail vein injection 100 mg/kg 5 consecutive days Evaluation of the therapeutic effect of Nelarabine in the acute T-lymphoblastic leukemia mouse model showed no significant difference in survival time between the Nelarabine group and the low- and medium-dose YLS010 groups. PMC11083707
Mice T-ALL patient-derived xenografts (PDXs) Intraperitoneal injection (IP) 125 mg/kg Days 0–4 and 14–18 Evaluate the in vivo efficacy of nelarabine alone or in combination with ACHM-025 against chemoresistant T-ALL PDX. Nelarabine alone significantly delayed leukemia progression, but when combined with ACHM-025, the disease was eradicated. PMC11542020
Mice B-ALL model Intraperitoneal injection 50 mg/kg 14 consecutive days Evaluate the therapeutic effect of EdC on the B-ALL model, showing significant reduction in leukemia burden and extended survival PMC11286238

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01094860 Leukemia PHASE1 COMPLETED 2018-08-09 University of Texas MD Anderso... More >>n Cancer Center, Houston, Texas, 77030, United States Less <<
NCT01376115 Cancer COMPLETED 2017-10-24 University of Tsukuba Hospital... More >>, Tsukuba, Japan Less <<
NCT00684619 T-ALL, T-NHL (Lymphoblastic) PHASE2 COMPLETED 2025-12-08 Robert Bosch Krankenhaus, Stut... More >>tgart, Baden-Württemberg, 70376, Germany|Klinikum der Universit?t Regensburg, Regensburg, Bayern, 93042, Germany|University Hospital of Frankfurt, Medical Dept. II, Frankfurt, Hessen, 60590, Germany|Medizinische Hochschule Hannover, Hannover, Niedersachsen, 30625, Germany|Universit?tsklinikum Essen, Essen, NRW, 45147, Germany|Universit?tsklinik Münster, Münster, NRW, 48149, Germany|Universit?tsklinik Dresden, Dresden, Sachsen, 01307, Germany|Universit?tsklinikum Leipzig, Leipzig, Sachsen, 04103, Germany|Universit?tsklinikum Kiel, Kiel, Schleswig-Holstein, 24105, Germany|Klinikum der FSU Jena, Jena, Thüringen, 07747, Germany|HELIOS Klinikum Berlin-Buch, Berlin, 13125, Germany Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.36mL

0.67mL

0.34mL

16.82mL

3.36mL

1.68mL

33.64mL

6.73mL

3.36mL

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