Nelarabine (Arranon; 506U78)

Alias: GW 506U78; 506 U 78; NSC-686673; 506 U78; GW-506U78; NS-686673; 506U78; GW506U78; Arranon; NSC686673

Cat No.:V1455 Purity: ≥98%

COA Product Data Instructions for use SDS

Nelarabine (formerly 506 U78; GW-506U78; NS-686673; 506U78; GW506U78; Atriance; Arranon; Nelzarabine) is a cytotoxic/chemotherapeutic medication approved for use in the treatment of hematological malignancies (T-cell acute lymphoblastic leukemia and T-cell lymphoblastic lymphoma).

Nelarabine (Arranon; 506U78) Chemical Structure CAS No.: 121032-29-9
Product category: DNA(RNA) Synthesis

This product is for research use only, not for human use. We do not sell to patients.

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Nature 2021, 597(7874):119-125.

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information

Product Description

Nelarabine (formerly 506 U78; GW-506U78; NS-686673; 506U78, GW506U78; Atriance; Arranon; Nelzarabine) is a cytotoxic/chemotherapeutic medication approved for use in the treatment of hematological malignancies (T-cell acute lymphoblastic leukemia and T-cell lymphoblastic lymphoma). It is an analog of purine nucleosides that inhibits DNA synthesis in tumor cells, with an IC50 ranging from 0.067 to 2.15 μM.

Biological Activity I Assay Protocols (From Reference)

Targets

DNA synthesis ( IC50 = 67 nM ); DNA synthesis (HSB2 cells) ( IC50 = 0.44 μM ); DNA synthesis (ALL-SIL cells) ( IC50 = 1.24 μM ); DNA synthesis (JURKAT cells) ( IC50 = 2.15 μM )

ln Vitro

Nelarabine has an IC50 that is 25 times and 113 times higher in the T- and B-lineages, respectively, than ARAC. Although there is significant overlap, T-ALL cells are eight times more sensitive to nerabine than B-lineage cells. NEL is 25 times less effective than ARAC in T-lineage and B-lineage cell lines, respectively.[1] Nelarabine works by preventing DNA synthesis and triggering cell death in vulnerable organisms[2]. Nelarabine showed notable antitumor activity while maintaining a manageable level of toxicity.[3]

ln Vivo

The AUC for ara-G plasma is 20 mM minutes, and the AUC for Nelarabine plasma is 2.82 mM minutes. Nelarabine in plasma has a terminal half-life of 25 minutes, a central volume of distribution of 1.1 L/kg, and a clearance of 42 mL/minutes/kg. Ara-G has a central volume of distribution of 1.4 L/kg and a terminal half-life of 182 minutes in plasma. Nelarabine and ara-G have terminal half-lives of 77 and 232 minutes, respectively, in CSF. AUCcsf:AUCplasma for ara-G is 23%, and for Nelarabine it is 29%. Due to their comparatively short half-lives, elarabine and ara-G do not accumulate with daily infusions.[4]

Cell Assay

The MTT assay is used to assess drug resistance in the HSB2, ALL-SIL, JURKAT, and PER-255 cell lines. After four days of incubation, elsarabine's concentration is examined in triplicate. The drug resistance metric known as the IC50, or drug concentration that inhibits cell growth by 50%, is employed. The data show the average of two to six separate experiments conducted at different times. When even the highest dose in a given experiment fails to produce 50% cytotoxicity, the IC50 is noted as being double the highest concentration that was tested.

Animal Protocol

35 mg/kg; i.v. injection

Healthy adult male rhesus monkeys

References

[1]. Br J Haematol . 2007 Apr;137(2):109-16.

[2]. Expert Opin Pharmacother . 2006 Sep;7(13):1791-9.

[3]. Blood . 2007 Jun 15;109(12):5136-42.

[4]. Cancer Chemother Pharmacol . 2007 May;59(6):743-7.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C11H15N5O5

Molecular Weight

297.27

Exact Mass

297.11

Elemental Analysis

C, 44.44; H, 5.09; N, 23.56; O, 26.91

CAS #

121032-29-9

Related CAS #

121032-29-9

Appearance

Solid powder

SMILES

COC1=NC(=NC2=C1N=CN2[C@H]3[C@H]([C@@H]([C@H](O3)CO)O)O)N

InChi Key

IXOXBSCIXZEQEQ-UHTZMRCNSA-N

InChi Code

InChI=1S/C11H15N5O5/c1-20-9-5-8(14-11(12)15-9)16(3-13-5)10-7(19)6(18)4(2-17)21-10/h3-4,6-7,10,17-19H,2H2,1H3,(H2,12,14,15)/t4-,6-,7+,10-/m1/s1

Chemical Name

(2R,3S,4S,5R)-2-(2-amino-6-methoxypurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-dio

Synonyms

GW 506U78; 506 U 78; NSC-686673; 506 U78; GW-506U78; NS-686673; 506U78; GW506U78; Arranon; NSC686673

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: ~60 mg/mL (~201.8 mM)

Water: ~3 mg/mL (~10.1 mM)

Ethanol: <1 mg/mL

Solubility (In Vivo)

1%DMSO+30% polyethylene glycol+1%Tween 80: 30 mg/mL

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.3639 mL	16.8197 mL	33.6395 mL
	5 mM	0.6728 mL	3.3639 mL	6.7279 mL
	10 mM	0.3364 mL	1.6820 mL	3.3639 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02619630	Recruiting	Drug: nelarabine	RT-cell Adult Acute Lymphoblastic Leukemia	Assistance Publique - Hôpitaux de Paris	December 2015	Phase 2
NCT00501826	Recruiting	Drug: Cytarabine Drug: Nelarabine	T Acute Lymphoblastic Leukemia T Lymphoblastic Lymphoma	M.D. Anderson Cancer Center	July 11, 2007	Phase 2
NCT01085617	Active Recruiting	Drug: nelarabine Drug: methotrexate	Leukemia Mucositis	University College, London	December 2010	Phase 3
NCT02881086	Active Recruiting	Drug: Nelarabine Drug: PEG-Asparaginase	Acute Lymphoblastic Leukemia Lymphoblastic Lymphoma	Goethe University	August 2016	Phase 3