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Tariquidar Chemical Structure

Tariquidar

Data Sheet For research use only. Not for human use.
Cat. No. :BCP06102CAS No. :206873-63-4Purity:98%
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  • Chemical Properties&Biological Activity
CAS No. 206873-63-4 Cat. No. BCP06102
Name Tariquidar
Synonyms XR 9576;XR-9576;XR9576;
SMILES
Chemical Name
Formula C38H38N4O6 M. Wt 646.73
Purity 98% Storage Store at 4-8°C
Description Tariquidar displays high-affinity binding to P-gp with Bmax of 275 pmol/mg. Tariquidar shows non-competitive interaction with the P-gp substrates vinblastine and paclitaxel. Tariquidar increases the steady-state accumulation of these cytotoxics in CHr<>/supB30 cells to levels observed in non-P-gp-expressing AuxB1 cells with EC50 of 487 nM. Tariquidar is able to inhibit the vanadate-sensitive ATPase activity of P-gp by 60-70%, with potent IC50 values of 43 nM. Tariquidar may inhibit other resistance mechanisms at higher concentrations. 1 μM Tariquidar abrogates ABCG2 (BCRP)-mediated resistance to camptothecins in vitro. Tariquidar potentiates the cyto-toxicity of several drugs including doxorubicin, paclitaxel, etoposide, and vincristine; complete reversal of resistance is achieved in the presence of 25- 80 nM Tariquidar. In MC26, a murine colon carcinoma cell line with intrinsic chemoresistance, the doxorubicin IC50 is fivefold lower in the presence of 0.1 μM Tariquidar (36 vs 7 nM).
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