Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD-5991 is a potent and selective Mcl-1 inhibitor (IC50: 0.7 nM in FRET assay; Kd: 0.17 nM in SPR assay).
ターゲット&IC50 | MCL1:0.17 nM (kd), MCL1:0.7 nM |
In vivo | Administration of a single intravenous (i.v.) dose of AZD5991 results in a dose-dependant antitumor effect, varying from tumor growth inhibition (TGI) to complete tumor regression (TR). Specifically, 10 days post-treatment, TGI is observed at 52% and 93% for doses of 10 and 30 mg/kg respectively. Remarkably, at a dose of 60 mg/kg, 99% TR is achieved with no detectable tumors in 6 of 7 mice, and at 100 mg/kg, complete TR is observed in all mice treated. Furthermore, AZD5991 demonstrates a dose-dependent duration of response, with tumors at the 100 mg/kg dose regrowing later than those at the 60 mg/kg dose. The efficacy of AZD5991 in vivo directly correlates with the activation of caspase-3 within the tumor and the drug's plasma concentration. The compound is well-tolerated across all dosages without significant weight loss in treated mice. A notable observation is the sustained effect of AZD5991, where a second dose administered 36 days following the initial dose induces tumor regression in all treated mice. Additionally, consecutive dosing at 100 mg/kg on days 0 and 1 results in a longer delay in tumor regrowth compared to a single dose at the same concentration, showcasing the compound's potent and durable antitumor activity. |
分子量 | 672.26 |
分子式 | C35H34ClN5O3S2 |
CAS No. | 2143061-81-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/mL (37.19 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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AZD-5991 2143061-81-6 Apoptosis BCL AZD 5991 AZD5991 Inhibitor inhibitor inhibit