Metagone Biotech Inc.

Yun Yu

Yi-Ta Tsai

Tai-Lung Cha

Sheng-Chieh Lin

Tai-Wei Ly

Disclosed herein is a compound of formula (I), which is ammonium salt of GW5074, wherein R, R, and Rare independently hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; or R, R, Rand the nitrogen are taken together to form a 6-membered heterocyclyl; and the alkyl, the alkenyl, the alkynyl, the aryl, the heteroaryl, or the 6-membered heterocyclyl is optionally substituted with at least one substituent selected from the group consisting of, &#x2014;OH, &#x2014;NH, and &#x2014;NRR, in which Rand Rare independently alkyl, aryl, or heteroaryl. Also disclosed herein is a pharmaceutical kit for the treatment of cancers. The pharmaceutical kit includes, a first formulation comprising a c-Raf inhibitor and a pharmaceutically acceptable carrier; and a second formulation comprising the compound of formula (I) and a pharmaceutically acceptable carrier. Also encompasses herein is a method of treating a subject having a cancer. The method comprises: (a) detecting whether the cancer cells of the subject has phosphorylation on serine 308 of death-associated protein kinase (DAPK); and (b) treating the subject based on the detection of the step (a) by, administering to the subject (i) an effective amount of a c-Raf inhibitor, and (ii) an effective amount of the compound of formula (I), when the phosphorylation on serine 308 of DAPK in the cancer cells is detected.

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Taipei, Taiwan

Yun Yu