2. Cell Cycle/DNA Damage Antibody-drug Conjugate/ADC Related
  3. Topoisomerase Antibody-Drug Conjugates (ADCs)
  4. DTS-108

DTS-108 是一种 SN38 (HY-13704) (一种拓扑异构酶 I 抑制剂) 的前药。DTS-108 是一种通过酯酶敏感的交联剂将 SN38 与人类寡肽连接而生成的偶联物。DTS-108 对结直肠癌、肺癌和乳腺癌具有抗癌活性。

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DTS-108 Chemical Structure

DTS-108 Chemical Structure

CAS No. : 951792-83-9

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DTS-108 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38 to a human oligopeptide via an esterase sensitive cross-linker. DTS-108 exhibits anti-tumor activity against colorectal, lung, and mammary cancer[1][2].

IC50 & Target[2]

Top1

 

体外研究
(In Vitro)

DTS-108 (48 h) 对结肠癌 (HCT 116、HT-29 和 LS 174T)、肺癌 (NCI-H460) 和乳腺癌 (MDA-MB-231)细胞株具有细胞毒性，IC50 分别为 24、94、2、40 和 834 nM[1]。
DTS-108 (2.55 μM, 0-48 h) 在人和狗血浆中的半衰期分别为 400 和 290 min，优于在小鼠血浆中的半衰期 (半衰期小于 3 min)[1]。

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

DTS-108 相关抗体:
体内研究
(In Vivo)

DTS-108 在剂量为 5 或 10 mg/kg 时对狗的毒性并不明显，只是狗的白细胞计数会出现中度下降，但并非剂量依赖性下降[1]。
DTS-108 (32-95 mg/kg, 静脉注射, 在第 3、7和11天) 在人肿瘤异种移植模型 (HCT116) 中剂量依赖性抗肿瘤，有一个10%的最小 T/C 比 (在 95 mg/kg 剂量下)[1]。
DTS-108 (静脉注射) 对植入结直肠癌、肺癌和乳腺癌细胞的裸鼠 (80 mg/kg，在第 3、5、7、10、12、14、17、19 和 21 天) 和植入结直肠癌细胞的大鼠 (63 mg/kg，在第 14、18、21、25 和 29 天) 具有抗肿瘤活性[1]。
DTS-108 (40 mg/kg, 静脉注射) 在携带人类 HT-29 细胞的结肠癌小鼠中抗肿瘤，并且与 5-FU (HY-90006) (40 mg/kg) 或贝伐珠单抗 (HY-P9906) (2 mg/kg) 联合使用时功效增加[1]。

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

Animal Model: Nude mice implanted into HT-29 (1 × 107) [1]
Dosage: 40 mg/kg
Administration: Intravenous injection (i.v.), on days 3, 6, 10, 13, 17, and 20 (with 5-FU); on days 3, 7, 11, 17, 21, and 25 (with bevacizumab)
Result: Exhibited anti-tumor activity in colon cancer mice bearing human HT-29 cells and has increased efficacy in combination with 5-FU or bevacizumab.
Animal Model: 7-wk-old female nude mice implanted into HCT 116 (1 × 107), NCI-H460 (3 × 106), MDA-MB-231 (3 × 106); Rh rnu/rnu nude rats implanted into LS 174T (2 × 107)[1]
Dosage: 80 mg/kg (mice); 63 mg/kg (rats)
Administration: Intravenous injection (i.v.), on days 3, 5, 7, 10, 12, 14, 17, 19, and 21 (mice); on days 14, 18, 21, 25, and 29 (rats)
Result: Exhibited anti-tumor activity in nude mice implanted with HCT 116, NCI-H460, and MDA-MB-231 cells, with minimum T/C ratios of 3%, 23%, and 29%, respectively.
Exhibited antitumoral efficacy (with a minimal T/C ratio of 44%) in rats bearing LS 174T.
分子量

3170.80

Formula

C145H233N43O33S2
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-108 相关分类

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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-108951792-83-9DTS108DTS 108TopoisomeraseAntibody-Drug Conjugates (ADCs)Antibody-Drug ConjugatesCytotoxicityMTDXenograftHCT 116Colorectal carcinomasNude miceAntitumoralInhibitorinhibitorinhibit

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