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Medchemexpress LLC Atrasentan | 173937-91-2 | C29H38N2O6 | 25 MG
Supplier: Medchemexpress LLC 25MGHY15403
Atrasentan (ABT-627) is an endothelin receptor antagonist with an IC50 of 0.0551 nM for ETA. It significantly inhibits LNCaP and C4-2b prostate cancer cell growth in vitro and demonstrates anti-tumor effects in vivo. It also induces several CYPs and acts as a moderate P-gp inhibitor.
- Endothelin A receptor antagonist with an IC50 of 0.0551 nM for ETA
- Inhibits LNCaP and C4-2b prostate cancer cell growth
- Elicits greater loss of viable prostate cancer cells when combined with Taxotere
- Down-regulates NF-κB DNA binding activity
- Induces several CYPs and drug transporters (e.g., CYP3A4)
- Moderate P-gp inhibitor (IC50 = 15.1 ± 1.6 μM in P388/dx cells)
- Weak BCRP inhibitor (IC50 = 59.8 ± 11 μM in MDCKII-BCRP cells)
- Inhibits pressor response induced by big endothelin-1 in pithed rats
- Inhibits C4-2b tumor growth within the bone environment in the SCID-hu model
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