Nelarabine

Research use only, not for human use.

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

Nelarabine is a purine nucleoside analog that is used as a cytotoxic agent in hematological malignancies. Nelarabine is converted into arabinosyl-guanine (ara-G) in the blood, and ara-G is selectively accumulated in T cells and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into DNA.(In Vitro):Nelarabine (506U78) (0-20 μM; 48 h) induces cytotoxic effects in T-ALL cell lines.Nelarabine (5 or 2 μM; 48 h) promotes apoptosis in sensitive T-ALL cell lines and modulates PI3K/AKT/mTOR and MEK signaling.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.(In Vivo):Nelarabine (506U78) (130 mg/kg/day; i.v.; 5 days) reduces leukemic burden and extends mouse survival in NSG mice xenografted with luciferase-expressing U937 cells.

Nelarabine (506U78) (0-20 μM; 48 h) induces cytotoxic effects in T-ALL cell lines.Nelarabine (5 or 2 μM; 48 h) promotes apoptosis in sensitive T-ALL cell lines and modulates PI3K/AKT/mTOR and MEK signaling.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. Cell Viability Assay Cell Line:T-ALL cell lines Concentration:0-20 μM Incubation Time:48 h 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).Apoptosis Analysis Cell Line:MOLT-4, JURKAT, P12-ICHIKAWA and DND41 Concentration:5 μM (2 μM for MOLT-4 cells)Incubation Time:48 h Result:Detected a marked increase in the percentage of early apoptotic and/or late apoptotic cells.Western Blot Analysis Cell Line:MOLT-4, JURKAT, P12-ICHIKAWA and DND41 Concentration:5 μM (2 μM for MOLT-4 cells)Incubation Time:0, 6, 16, 24 and 48 h Result:Documented a time-dependent cleavage of caspase 8, caspase 9, caspase 3, and poly(ADP-ribose) polymerase (PARP) in response to drug treatment.

Nelarabine (506U78) (130 mg/kg/day; i.v.; 5 days) reduces leukemic burden and extends mouse survival in NSG mice xenografted with luciferase-expressing U937 cells. Animal Model:NSG mice xenografted with luciferase-expressing U937 cells Dosage:130 mg/kg/day Administration:Intravenous injection, 5 days Result:Reduced leukemic burden and extended mouse survival.

Arranon, 506U78, GW506U78 | GW-506U78

Immunology/Inflammation

TLR

DNA synthesis (ALL-SIL cells)| DNA synthesis (HSB2 cells)| DNA synthesis (JURKAT cells)| DNA synthesis (PER-255 cells)

Cancer

——

121032-29-9

297.27

C11H15N5O5

>98% (HPLC)

DMSO : 9.8 mg/mL. 32.97 mM;

COC1=NC(N)=NC2=C1N=CN2[C@@H]1O[C@H](CO)[C@@H](O)[C@@H]1O

(2R,3S,4R,5R)-2-(2-amino-6-methoxy-9H-purin-9-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol

(-20℃)

With Ice Pack

≥ 2 years