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| Product | Description | |
|---|---|---|
| CKD-516 | This active molecular is a tubulin polymerisation inhibitor which is applicated for solid cancer treatment. CKD-516 disruptes tubulin of the endothelial cytoskeleton selectively. In Jun 2012, a South Korea company, Chong Kun Dang initiated enrolment in a phase I trial for solid tumours treatment in South Korea. In Dec 2014, Phase-I clinical trials in Solid tumours in South Korea was on going. Uses: Solid tumours. Synonyms: CKD-516 HCl; CKD 516 HCl; CKD516 HCl; (2S)-2-amino-3-methyl-N-[4-[3-(1,2,4-triazol-1-yl)-4-(3,4,5-trimethoxybenzoyl)phenyl]-1,3-thiazol-2-yl]butanamide;hydrochloride;1188371-47-2 (free base). Grades: 98%. CAS No. 1188371-47-2. Molecular formula: C26H28N6O5S. Mole weight: 536.6. |  |
| CKD-516 HCl | CKD-516 is tubulin inhibitor for solid cancer, which was initiated phase 1 trial in Korea in 2010. CKD-516 selectively disrupted tubulin component of the endothelial cytoskeleton. Serial DCE-MRI showed a significant decrease in K-trans and IAUGC parameters from baseline at 4 h (39.9 % in K-trans; -45.0 % in IAUGC) and at 24 h (-32.2 % in K-trans; -36.5 % in IAUGC), and a significant recovery at 48 h (22.9 % in K-trans; 34.8 % in IAUGC) following administration of CKD-516 at a 0.7-mg/kg dose. When the tumors were stratified according to the initial K-trans value of 0.1, tumors with a high K-trans?>?0.1 which was indicative of having well-developed pre-existing vessels, showed greater reduction in K-trans and IAUGC values. On histologic examination, the degree of necrosis of treated tumors was significantly greater than that of untreated tumors. In summary, CKD-516 is an effective VDA which results in rapid vascular shutdown by targeting the tubulin component of tumor vessels and thus leads to necrosis. Synonyms: Valecobulin hydrochloride; CKD516 hydrochloride; CKD 516 hydrochloride. CAS No. 1240321-53-2. Molecular formula: C26H29ClN6O5S. Mole weight: 573.07. | |
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