Bioactivity | XR9051 hydrochloride is an orally active and specific modulator of P-glycoprotein-mediated multidrug resistance (MDR)[1]. |
Invitro | XR9051 is able to reverse resistance to a variety of cytotoxic drugs, including doxorubicin, etoposide and vincristine, which are associated with classical MDR[1].XR9051 is highly active and gave at least a 15- to 20- fold decrease in the doxorubicin IC50, in the acquired resistance cell lines[1]. |
In Vivo | XR9051 (20-40 mg/kg, ip) shows significant modulatory activity in mice bearing MDR human ovarian (2780AD and CH1/DOXr) and SCLC (H69/LX) xenografts[2]. Animal Model: |
Name | XR9051 hydrochloride |
CAS | 180422-22-4 |
Formula | C39H39ClN4O5 |
Molar Mass | 679.20 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. I L Dale , et al. Reversal of P-glycoprotein-mediated multidrug resistance by XR9051, a novel diketopiperazine derivative. Br J Cancer. 1998 Oct;78(7):885-92. [2]. P Mistry, et al. In vivo efficacy of XR9051, a potent modulator of P-glycoprotein mediated multidrug resistance. Br J Cancer. 1999 Apr;79(11-12):1672-8. |