Nelarabine

ArtNr	S1213-200
Hersteller	Selleckchem
CAS-Nr.	121032-29-9
Menge	200 mg
Quantity options	10 mg 100 mg 1 g 10 g 10 mM/1 mL 200 mg 25 mg 5 mg 50 mg 5 g
Kategorie	Oncology Food Safety Drugs Inhibitors & Compound Libraries Small Molecules By Organ Skin Cancer Heart & Blood Cancer Lymphatic System Cancer
Typ	Inhibitors
Specific against	other
Smiles	COC1=NC(=NC2=C1N=CN2C3C(C(C(O3)CO)O)O)N
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	506U78,Arranon
Similar products	Nelarabine
Lieferbar
Storage Conditions	2 years -80 in solvent
Molecular Weight	297, 27
Administration	Administered via i.v.
Animal Models	Healthy adult male rhesus monkeys
Cell lines	HSB2, ALL-SIL, JURKAT and PER-255 cell lines
Clinical Trials	Nelarabine plus Doxorubicin, Cyclophosphamide, Cytarabine, Dexamethasone, Methotrexate or Vincristine has entered in a phase II clinical trial in the treatment of leukemia, acute lymphoblastic leukemia, and lymphoblastic lymphoma.
Concentrations	0.125 ug/mL - 8 ug/mL
Dosages	35 mg/kg
Formulation	Control
IC50	0.13 ug/mL, 0.13 ug/mL, 0.13 ug/mL, 0.13 ug/mL, 0.13 ug/mL, 0.13 ug/mL
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]
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 2â€“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.
Solubility (25C)	DMSO 60 mg/mL, Water 3 mg/mL, Ethanol <1 mg/mL
Information	Nelarabine (506U78, Arranon) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.
Features	Nelarabine is rapidly converted into ara-G through demethoxylation by adenosine deaminase.

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