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Nelarabine

Catalog No. T6603 CAS 121032-29-9

Synonyms: GW 506U78, Nelzarabine, 506U78

Nelarabine (GW 506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.

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Nelarabine, CAS 121032-29-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 52.00
5 mg	In stock	$ 81.00
10 mg	In stock	$ 143.00
25 mg	In stock	$ 259.00
50 mg	In stock	$ 459.00
100 mg	In stock	$ 578.00
500 mg	In stock	$ 1,220.00
1 mL * 10 mM (in DMSO)	In stock	$ 81.00

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Purity: 99.6%

Purity: 97.90%

Biological Description

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Storage & Solubility Information

Description	Nelarabine (GW 506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.
Targets&IC50	DNA synthesis (PER-255 cells):0.067-2.15 μM
In vitro	The IC50 of Nelarabine is 25-fold and 113-fold higher than ARAC in T- and B-lineage, respectively. T-ALL cells are eightfold more sensitive to Nelarabine than B-lineage but there is considerable overlap. The efficacy of NEL in T-lineage and B-lineage cell lines is 25-fold and 113-fold less than ARAC, respectively. [1] Nelarabine acts by inhibiting DNA synthesis and inducing apoptosis in susceptible cells. [2]Nelarabine demonstrated significant antineoplastic activity with acceptable toxicity. [3]
In vivo	The Nelarabine plasma AUC is 2.82 mM minutes and the ara-G plasma AUC is 20 mM minutes. The terminal half-life of Nelarabine in plasma is 25 min, clearance is 42 mL/minutes/kg, and central volume of distribution is 1.1 L/kg. The terminal half-life of ara-G in plasma is 182 minutes and the central volume of distribution is 1.4 L/kg. In CSF the terminal half-life of Nelarabine is 77 minutes and of ara-G is 232 minutes. The AUCcsf:AUCplasma is 29 % for Nelarabine and 23 % for ara-G. Nelarabine and ara-G do not accumulate with daily infusions because of their relatively short half-lives. [4]
Cell Research	HSB2, ALL-SIL, JURKAT and PER-255 cell lines are tested for drug resistance using the MTT assay. Nelarabine are incubated over 4 days, with concentration tested in triplicate. The IC50 (drug concentration that inhibits cell growth by 50%) is used as the measure of drug resistance. Data represent the average of 2-6 experiments performed on separate occasions. In cases where 50% cytotoxicity is not achieved by even the highest dose in a particular experiment, the IC50 is recorded as double the highest concentration tested.(Only for Reference)

Synonyms	GW 506U78, Nelzarabine, 506U78
Molecular Weight	297.27
Formula	C11H15N5O5
CAS No.	121032-29-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 3 mg/mL (10 mM)), Heating is recommended.

DMSO: 29.7 mg/mL (100 mM)

References and Literature

1. Beesley AH, et al. Br J Haematol. 2007, 137(2), 109-116. 2. Kline J, et al. Expert Opin Pharmacother. 2006, 7(13), 1791-1799. 3. DeAngelo DJ, et al. Blood. 2007, 109(12), 5136-5142. 4. Berg SL, et al. Cancer Chemother Pharmacol. 2007, 59(6), 743-747.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library EMA Approved Drug Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Bioactive Compound Library Cell Cycle Compound Library Pediatric Drug Library

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Keywords

Nelarabine 121032-29-9 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair Nucleoside Antimetabolite/Analog DNA/RNA Synthesis HSB-2 Inhibitor T-ALL GW 506U78 acute lymphoblastic leukaemia MOLT-4 P12 DND41 Nelzarabine inhibit 506U78 JURKAT inhibitor

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