| Chemical Name |
Atrasentan |
| CAS Number |
173937-91-2 |
| MDL Number |
MFCD00940177 |
| Molecular Formula |
C29H38N2O6 |
| Molecular Weight |
510.62 |
| Synonyms |
ABT-627;(+)-A 127722;A-147627 |
Introduction of 173937-91-2 :
Atrasentan (ABT-627) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA[1]. IC50 & Target: IC50: 0.055 nM (ETA) In Vitro: Atrasentan (ABT-627, 0-50 μM) significantly inhibits LNCaP and C4-2b prostate cancer cell growth. ABT-627 in conbination with Taxotere elicits a significantly greater loss of viable prostate cancer cells relative to either agent alone and shows greater degree of down-regulation of the NF-κB DNA binding activity[2]. Atrasentan profoundly induces several CYPs and drug transporters (e.g. 12-fold induction of CYP3A4 at 50 μM). It is a moderate P-gp inhibitor (IC50 in P388/dx cells=15.1±1.6 μM) and a weak BCRP inhibitor (IC50 in MDCKII-BCRP cells=59.8±11 μM)[3]. In Vivo: Atrasentan (3 mg/kg, p.o.) inhibits the pressor response induced by big endothelin-1 (1 nmol/kg) in pithed rats[1]. Aatrasentan (ABT-627, 10 mg/kg, i.p.) as well as Taxotere alone inhibited the C4-2b tumor growth within the bone environment to some extent in the SCID-hu model[2].
| Purity |
NLT 98% |
| Storage |
at 20ºC 2 years |
*The above information is for reference only.
