Nelarabine

Name: Nelarabine
Brand: Selleckchem
SKU: S1213

Description

Nelarabine

Catalog No.S1213

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

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Description	Nelarabine is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.
Targets	DNA (HSB2 cell lines)	DNA (ALL-SIL cell lines)	DNA (JURKAT cell lines)	DNA (PER-255 cell lines)
IC50	0.44 μM	1.24 μM	2.15 μM	0.067 μM ^[1]
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]
Features	Nelarabine is rapidly converted into ara-G through demethoxylation by adenosine deaminase.

Cell lines	HSB2, ALL-SIL, JURKAT and PER-255 cell lines
Concentrations	0.125 μg/mL - 8 μg/mL
Incubation Time	96 hours
Method	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.

Animal Models	Healthy adult male rhesus monkeys
Dosages	35 mg/kg
Administration	Administered via i.v.
Solubility	1% DMSO/30% polyethylene glycol/1% Tween 80, 30 mg/mL

Solubility (25°C) *	In vitro	DMSO	60 mg/mL (201 mM)
		Water	3 mg/mL (10 mM)
		Ethanol	<1 mg/mL (<1 mM)
	In vivo	1% DMSO/30% polyethylene glycol/1% Tween 80,	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.