Nelarabine
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).
For research use only. We do not sell to patients.
- Purity: 99.76%
- CAS No.: 121032-29-9
- Formula: C11H15N5O5
- Molecular Weight:297.27
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Nelarabine
More
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-HSB-2 | IC50 |
0.067 μM
Compound: 17
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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
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[PMID: 33540357] |
| Jurkat | IC50 |
0.067 μM
Compound: 17
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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
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[PMID: 33540357] |
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.
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Cell Line:T-ALL cell lines
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Concentration:0-20 μM
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Incubation Time:48 h
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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).
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Cell Line:MOLT-4, JURKAT, P12-ICHIKAWA and DND41
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Concentration:5 μM (2 μM for MOLT-4 cells)
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Incubation Time:48 h
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Result:Detected a marked increase in the percentage of early apoptotic and/or late apoptotic cells.
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Cell Line:MOLT-4, JURKAT, P12-ICHIKAWA and DND41
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Concentration:5 μM (2 μM for MOLT-4 cells)
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Incubation Time:0, 6, 16, 24 and 48 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice xenografted with luciferase-expressing U937 cells[2]
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Dosage:130 mg/kg/day
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Administration:Intravenous injection, 5 days
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Result:Reduced leukemic burden and extended mouse survival.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 121032-29-9
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Appearance Solid
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Molecular Weight 297.27
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Formula C11H15N5O5
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Color White to off-white
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SMILES
OC[C@@H]1[C@@H](O)[C@H](O)[C@H](N2C=NC3=C(OC)N=C(N)N=C23)O1
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Synonyms
506U78; GW 506U78; Nelzarabine
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
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Most Recent
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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)
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 May 8:769:151971. PMID: 40354678
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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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)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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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