| Bioactivity | DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer[1]. |
| In Vivo | DTS-201 (小鼠为 40-100 mg/kg、大鼠为 30-70 mg/kg、狗为 4-8 mg/kg，静脉注射，15 min) sodium 在小鼠、大鼠和狗中耐受性良好[1]。DTS-201 (静脉注射，15 min，在第 1 天和第 22 天) sodium 在小鼠 (50 mg/kg，MTD) 和大鼠 (40 mg/kg，MTD) 中耐受性良好[1]。DTS-201 (3.2、12.8 和 25.6 mg/kg，静脉注射，每周一次，连续 7 周) sodium 对心脏的毒性明显小于 Doxorubicin, 无论剂量水平如何，平均总分均小于等于 0.3[1]。DTS-201 (40-80 mg/kg，静脉注射) sodium 在 NCI-H1299、PC-3 和 MDA-MB-231 异种移植小鼠中比游离 Doxorubicin 有更好的治疗指数[1]。DTS-201 sodium 以不断增加的剂量给比格犬静脉注射 15 min后的毒物动力学结果 hERG IC50Dose (mg/kg) |
| CAS | 372491-73-1 |
| Formula | C49H64N5NaO18 |
| Molar Mass | 1034.04 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Ravel D, et al. Preclinical toxicity, toxicokinetics, and antitumoral efficacy studies of DTS-201, a tumor-selective peptidic prodrug of doxorubicin. Clinical cancer research : an official journal of the American Association for Cancer Research. 2008, 14(4), 1258–1265. |
DTS-201 sodium
CAS: 372491-73-1 F: C49H64N5NaO18 W: 1034.04
DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide porti
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