IITZ-01

IITZ-01 是一种有效的溶酶体自噬抑制剂，具有单剂抗肿瘤活性，对 PI3Kγ 的 IC50 为 2.62 μM。

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库存: 现货

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数量
5mg

￥762.00

610.00

- +
10mg

￥1412.00

1130.00

- +
25mg

￥2825.00

2260.00

- +
50mg

￥4700.00

3760.00

- +
100mg

￥7012.00

5610.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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Background

IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.

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].

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].

[1]. Guntuku L, et al. IITZ-01, a novel potent lysosomotropic autophagy inhibitor, has single-agent antitumor efficacy in triple-negative breast cancer in vitro and in vivo. Oncogene. 2018 Aug 30.