Name | IITZ-01 |
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Description | IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ. |
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Related Catalog | |
Target |
PI3Kγ:2.62 μM (IC50) Autophagy |
In Vitro | IITZ-01 shows negligible inhibition toward PI3Kγ (IC50: 2.62μM). Time-course immunoblotting experiment with IITZ-01-treated cells also displays significant elevation in SQSTM1 levels, indicating the autophagy inhibitory nature of the compound. In addition to that, both compounds IITZ-01 has demonstrated potent autophagy inhibitory activity in other breast, lung, and colon cancer cells[1]. |
In Vivo | Tumors after reaching ~100 mm3, vehicle, 45 mg/kg of IITZ-01, is administered through intraperitoneal (i.p.) route on every alternate day for 4 weeks. IITZ-01 reduces the active tumor burden around 8.8-fold, when compared with control group as determined by tumor photon counts. Moreover, tumor volume measurements have demonstrated that IITZ-01 has significantly inhibited average tumor growth when compared with control from third day of treatment. Significant reduction in average tumor weights is observed after treatment with IITZ-01 compared with control. This treatment schedule of both compounds is well tolerated in mice for the total duration of administration with no significant changes in their body weights[1]. |
References |
Molecular Formula | C26H23FN8O |
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Molecular Weight | 482.51 |
Storage condition | 2-8℃ |