| Bioactivity | 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]. |
| Invitro | 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. 0 --> DTS-108 相关抗体: |
| 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: |
| CAS | 951792-83-9 |
| Formula | C145H233N43O33S2 |
| Molar Mass | 3170.80 |
| 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]. Meyer-Losic, et al. DTS-108, a novel peptidic prodrug of SN38: in vivo efficacy and toxicokinetic studies. Clinical cancer research : an official journal of the American Association for Cancer Research. 2008, 14(7), 2145–2153. [2]. Coriat, et al. Pharmacokinetics and safety of DTS-108, a human oligopeptide bound to SN-38 with an esterase-sensitive cross-linker in patients with advanced malignancies: a Phase I study. International journal of nanomedicine. 2016, 11, 6207–6216. |
DTS-108
CAS: 951792-83-9 F: C145H233N43O33S2 W: 3170.80
DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38
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