1. Cell Cycle/DNA Damage Apoptosis
  2. Nucleoside Antimetabolite/Analog Apoptosis
  3. Nelarabine

Nelarabine  (Synonyms: 506U78; GW 506U78; Nelzarabine)

Cat. No.: HY-13701 Purity: 99.76%
Data Sheet SDS COA Handling Instructions

Nelarabine (506U78) is a nucleoside analogue and can be used for the research of T cell acute lymphoblastic leukemia (T-ALL).

For research use only. We do not sell to patients.

Nelarabine Chemical Structure

Nelarabine Chemical Structure

CAS No. : 121032-29-9

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Nelarabine (506U78) is a nucleoside analogue and can be used for the research of T cell acute lymphoblastic leukemia (T-ALL)[1].

Cellular Effect
Cell Line Type Value Description References
CCRF-HSB-2 IC50
0.067 μM
Compound: 17
Antiproliferative activity against human CCRF-HSB-2 cells assessed as cell growth inhibition incubated for 4 days by MTT assay
Antiproliferative activity against human CCRF-HSB-2 cells assessed as cell growth inhibition incubated for 4 days by MTT assay
[PMID: 33540357]
Jurkat IC50
0.067 μM
Compound: 17
Antiproliferative activity against human Jurkat cells assessed as cell growth inhibition incubated for 4 days by MTT assay
Antiproliferative activity against human Jurkat cells assessed as cell growth inhibition incubated for 4 days by MTT assay
[PMID: 33540357]
In Vitro

Nelarabine (506U78) (0-20 μM; 48 h) induces cytotoxic effects in T-ALL cell lines[1].
Nelarabine (5 or 2 μM; 48 h) promotes apoptosis in sensitive T-ALL cell lines and modulates PI3K/AKT/mTOR and MEK signaling[1].
Nelarabine (10 μM; 0-48 h) resistance does not depend on expression of ENT1/2 transporters and is partly due to upregulation of PI3K, MEK, and Bcl2 signaling[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: T-ALL cell lines
Concentration: 0-20 μM
Incubation Time: 48 h
Result: Cell viability decreased in a concentration-dependent fashion, and the IC50 values ranged between 2 and 5.5 μM for sensitive cell lines (MOLT-4, HSB-2, P12, DND41, JURKAT).

Apoptosis Analysis[1]

Cell Line: MOLT-4, JURKAT, P12-ICHIKAWA and DND41
Concentration: 5 μM (2 μM for MOLT-4 cells)
Incubation Time: 48 h
Result: Detected a marked increase in the percentage of early apoptotic and/or late apoptotic cells.

Western Blot Analysis[1]

Cell Line: MOLT-4, JURKAT, P12-ICHIKAWA and DND41
Concentration: 5 μM (2 μM for MOLT-4 cells)
Incubation Time: 0, 6, 16, 24 and 48 h
Result: Documented a time-dependent cleavage of caspase 8, caspase 9, caspase 3, and poly(ADP-ribose) polymerase (PARP) in response to drug treatment.
Induced a marked decrease of phosphorylated AKT at Ser473, S6 ribosomal protein (S6RP) at Ser235/236, and GSK3β at Ser9.
In Vivo

Nelarabine (506U78) (130 mg/kg/day; i.v.; 5 days) reduces leukemic burden and extends mouse survival in NSG mice xenografted with luciferase-expressing U937 cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NSG mice xenografted with luciferase-expressing U937 cells[2]
Dosage: 130 mg/kg/day
Administration: Intravenous injection, 5 days
Result: Reduced leukemic burden and extended mouse survival.
Clinical Trial
Molecular Weight

297.27

Formula

C11H15N5O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC[C@@H]1[C@@H](O)[C@H](O)[C@H](N2C=NC3=C(OC)N=C(N)N=C23)O1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (336.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 10 mg/mL (33.64 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3639 mL 16.8197 mL 33.6393 mL
5 mM 0.6728 mL 3.3639 mL 6.7279 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 5 mg/mL (16.82 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.76%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.3639 mL 16.8197 mL 33.6393 mL 84.0983 mL
5 mM 0.6728 mL 3.3639 mL 6.7279 mL 16.8197 mL
10 mM 0.3364 mL 1.6820 mL 3.3639 mL 8.4098 mL
15 mM 0.2243 mL 1.1213 mL 2.2426 mL 5.6066 mL
20 mM 0.1682 mL 0.8410 mL 1.6820 mL 4.2049 mL
25 mM 0.1346 mL 0.6728 mL 1.3456 mL 3.3639 mL
30 mM 0.1121 mL 0.5607 mL 1.1213 mL 2.8033 mL
DMSO 40 mM 0.0841 mL 0.4205 mL 0.8410 mL 2.1025 mL
50 mM 0.0673 mL 0.3364 mL 0.6728 mL 1.6820 mL
60 mM 0.0561 mL 0.2803 mL 0.5607 mL 1.4016 mL
80 mM 0.0420 mL 0.2102 mL 0.4205 mL 1.0512 mL
100 mM 0.0336 mL 0.1682 mL 0.3364 mL 0.8410 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Nelarabine
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