Cat. No.: HY-13701

Nelarabine

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

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

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

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Pureté: 99.76%
CAS No.: 121032-29-9
Formule: C₁₁H₁₅N₅O₅
Masse moléculaire:297.27

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Nelarabine Chemical Structure

CAS No.: 121032-29-9

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (3)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 121032-29-9
Appearance Solid
Masse moléculaire 297.27
Formule C₁₁H₁₅N₅O₅
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
Synonyms

506U78; GW 506U78; Nelzarabine
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
Biochem Biophys Res Commun

Connectivity-map unveils Gemcitabine's efficacy in overcoming nelarabine resistance in T-cell acute lymphoblastic leukemia. [Abstract]

2025 Jul 8:769:151971. PMID: 40354678

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3639 mL

16.8197 mL

33.6393 mL

5 mM

0.6728 mL

3.3639 mL

6.7279 mL

10 mM

0.3364 mL

1.6820 mL

3.3639 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Lonetti A, et al. Improving nelarabine efficacy in T cell acute lymphoblastic leukemia by targeting aberrant PI3K/AKT/mTOR signaling pathway. J Hematol Oncol. 2016 Oct 24;9(1):114. [Content Brief]

[2]. Wang H, et al. Repurposing Nelarabine to Induce Differentiation of Acute Myeloid Leukemia. Blood, 2020, 136: 26.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

Nelarabine

3 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Nelarabine

Activité biologique

Chemical Information

Publications (3)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Nelarabine Related Classifications

HY-13701 Related Classifications