Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
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.
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 )
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ln Vitro |
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ln Vivo |
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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.
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Animal Protocol |
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References |
Molecular Formula |
C11H15N5O5
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Molecular Weight |
297.27
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Exact Mass |
297.11
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Elemental Analysis |
C, 44.44; H, 5.09; N, 23.56; O, 26.91
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CAS # |
121032-29-9
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
COC1=NC(=NC2=C1N=CN2[C@H]3[C@H]([C@@H]([C@H](O3)CO)O)O)N
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InChi Key |
IXOXBSCIXZEQEQ-UHTZMRCNSA-N
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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
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Chemical Name |
(2R,3S,4S,5R)-2-(2-amino-6-methoxypurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-dio
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% DMSO +30% polyethylene glycol+1% Tween 80 : 30 mg/mL Solubility in Formulation 5: 5 mg/mL (16.82 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
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.
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.
(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.
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 |