8-Chloroadenosine

Research use only, not for human use.

8-Chloroadenosine is a 5' AMP-activated protein kinase agonist potentially for the treatment of chronic lymphocytic leukemia.

8-Chloroadenosine is a 5' AMP-activated protein kinase agonist potentially for the treatment of chronic lymphocytic leukemia. 8-chloroadenosine activity is associated with inhibition of the mTOR pathway.8-Chloroadenosine is a nucleoside analog; metabolized in vivo to 8-Chloro-ATP. Incorporates into RNA during transcription and inhibits RNA synthesis. Exhibits cytotoxicity in MM.1S, RPMI-8226, and U266 cancer cell lines; induces G2/M cell cycle arrest and mitotic catastrophe in A549 and H1299 cells. 8-Chloroadenosine has been shown to deplete ATP and inhibit tumor growth in hematological malignancies as well as in lung and breast cancer cell lines.

8-Chloroadenosine (8-Cl-Ado; 10 μM; 24-72 hours) induces an autophagic flux in both LC3B-II and p62 levels. 8-Chloroadenosine (10 μM; 7-21 hours) induces phosphorylation of AMPK (Thr172) in a time-dependent manner in MCF-7 and BT-474 cells. Total AMPK protein levels were unchanged. 8-Chloroadenosine readily induces the phosphorylation of raptor Ser792 in MCF-7 cells. 8-Chloroadenosine (10 μM; 4-72 hours) induces ULK1 phosphorylation on Ser555 in MCF-7 and BT-474 cells.8-Chloroadenosine attenuates mTOR activity in breast cancer cells. 8-Chloroadenosine is independent of p53. 8-Chloroadenosine (10 μM; 3 days) inhibits over 90% clonogenic survival in the MCF-7 breast cancer cell lines. The amount of apoptosis induction only reached ~30%. 8-Chloroadenosine (10 μM) treatment results in a rapid depletion of ATP within 12-hours in T47D, SK-BR-3, and ZR-75-1 cells.

8-Chloroadenosine (25-100 mg/kg; IP; three times a week for 3 weeks) inhibits growth of both MCF-7 and BT-474 xenograft tumors with 100 mg/kg. 8-Chloroadenosine with 50 mg/kg dose does not affect the growth of the BT-474 xenograft tumors.

8 Chloroadenosine | 8Chloroadenosine | NSC-354258 | NSC 354258 | NSC354258 | 8-Cl-Ado

Membrane Transporter/Ion Channel

AMPK

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34408-14-5

301.69

C10H12ClN5O4

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (414.33 mM)

Nc1ncnc2n([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c(Cl)nc12

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(-20℃)

With Ice Pack

≥ 2 years