2. Metabolic Enzyme/Protease
  3. Aminopeptidase
  4. DTS-201 sodium

DTS-201 sodium (CPI-0004Na) 是一种 Doxorubicin (HY-15142A) 的肽前药。DTS-201 包括四肽部分，在肿瘤环境中被内肽酶水解产生代谢物，继而进入细胞后转化为活性 Doxorubicin。DTS-201 在前列腺癌、乳腺癌和肺癌的肿瘤异种移植模型中显示出抗肿瘤疗效。

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Custom Peptide Synthesis

DTS-201 sodium Chemical Structure

DTS-201 sodium Chemical Structure

CAS No. : 372491-73-1

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DTS-201 sodium 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体内研究
(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) 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) 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) 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) 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 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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

hERG IC50Dose (mg/kg) Dose (μmol/kg) Cmax (μM) Tmax (min) AUC(0-t) (h ×μM)
4 3.9 14.4 15 5.1
8 7.8 42.6 15 15.7
16 15.5 83.6 15 38.2
32 31.0 209 15 127
Animal Model: Xenograft mouse models (seven-week-old male or female NMRI nu/nu mice were respectively injected with a PC-3 cell suspension (1 × 107 cells/mL) or a MDA-MB-231 suspension (6 × 107 cells/mL) in the ventral skin or implanted with a NCI-H1299 tumor fragment)[1]
Dosage: 40 mg/kg, 60 mg/kg, 80 mg/kg
Administration: Intraperitoneal injection (i.p.), weekly for 4 (NCI-H1299), 5 (PC-3), or 6 (MDA-MB-231) weeks
Result: Showed to be more active at 40 mg/kg than Doxorubicin at the end of the study (PC-3 prostate cancer model).
Showed a higher activity in the MDA-MB-231 breast tumor model compared with Doxorubicin, with treated versus control values of 25% and 43%, respectively.
Showed significant dose-dependent efficacy, with treated versus control values of 38% and 17%, respectively in the NCI-H1299 lung cancer model.
分子量

1034.04

Formula

C49H64N5NaO18
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DTS-201 sodium 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DTS-201372491-73-1DTS201DTS 201AminopeptidaseWBCMTDAntitumoralMDA-MB-231NCI-H1299Subchronic toxicityCardiac toxicityprostate cancerbreast cancerlung cancerInhibitorinhibitorinhibit

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