Conteltinib (CT-707) 是一种多激酶抑制剂，可靶向作用于 FAK，ALK 和 Pyk2。Conteltinib (CT-707) 对 FAK 具有显着的抑制作用，IC₅₀ 为 1.6 nM。

Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK, ALK, and Pyk2. Conteltinib exerts significant inhibitory effect on FAK with an IC 50 of 1.6 nM.

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IC50: 1.6 nM (FAK)

Conteltinib (CT-707) synergizes with XL184 to suppress hepatocellular carcinoma by blocking XL184-induced FAK activation.
The combination of XL184 (5 μM) and Conteltinib (3 μM) significantly reduces the survival fraction, compared with each agent alone.
The combination of XL184 (5 μM) and Conteltinib (3 μM) results in enhanced caspase-dependent apoptosis in human hepatocellular carcinoma cell lines.
The FAK phosphorylation induced by XL184 (5 μM) might be involved in the synergistic antitumor effect of Conteltinib (3 μM) and XL184. has not independently confirmed the accuracy of these methods. They are for reference only.

The combination of XL184 (20 mg/kg once daily for first 3 days; i.g. 10 mg/kg once a day for 4th day; no administration from 5th to 10th days; i.g. 10 mg/kg once a day from the 10th to 14th days )and CT-707 (i.g. 50 mg/kg twice a day for first 3 days, 7th, 8th, 11th, 12th, and 14th days; once a day for 4th, 6th, 9th, 10th, and 13th days; no administration for the 5th day) shows the synergistic antitumor effect in HepG2 xenograft nude mice. has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Wang DD, et al. CT-707, a Novel FAK Inhibitor, Synergizes with XL184 to Suppress Hepatocellular Carcinoma by Blocking XL184-Induced FAK Activation. Mol Cancer Ther. 2016 Dec;15(12):2916-2925.

In Vitro: DMSO : 31.25 mg/mL (49.15 mM; Need ultrasonic)配制储备液