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UNBS3157是一种新型的非血液毒性萘酰亚胺衍生物,具有强大的抗肿瘤活性,能够通过DNA插入作用和毒化拓扑异构酶IIalpha来与DNA结合。与之相关的萘酰亚胺类化合物Amonafide在二期乳腺癌试验中表现出了活性,但由于限制剂量的骨髓毒性,目前尚未进入三期临床试验。相比之下,UNBS3157的最大耐受剂量比Amonafide高出3-4倍,并且在显示出显著抗肿瘤效果的剂量下未引起小鼠的血液毒性。此外,在活体内模型中,包括(i) L1210鼠白血病、(ii) MXT-HI鼠乳腺腺癌、以及(iii)人类A549非小细胞肺癌和BxPC3胰腺癌原位模型中,UNBS3157显示出优于Amonafide的效果。
UNBS3157是一种新型的非血液毒性萘酰亚胺衍生物,具有强大的抗肿瘤活性,能够通过DNA插入作用和毒化拓扑异构酶IIalpha来与DNA结合。与之相关的萘酰亚胺类化合物Amonafide在二期乳腺癌试验中表现出了活性,但由于限制剂量的骨髓毒性,目前尚未进入三期临床试验。相比之下,UNBS3157的最大耐受剂量比Amonafide高出3-4倍,并且在显示出显著抗肿瘤效果的剂量下未引起小鼠的血液毒性。此外,在活体内模型中,包括(i) L1210鼠白血病、(ii) MXT-HI鼠乳腺腺癌、以及(iii)人类A549非小细胞肺癌和BxPC3胰腺癌原位模型中,UNBS3157显示出优于Amonafide的效果。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | 询价 | 10-14周 | |
50 mg | 询价 | 10-14周 |
产品描述 | UNBS3157 is a novel naphthalimide derivative that is non-hematotoxic and exhibits significant antitumor activity through DNA intercalation and the poisoning of topoisomerase IIalpha. Unlike Amonafide, a related naphthalimide compound that showed activity in Phase II breast cancer trials but did not proceed to Phase III due to dose-limiting myelotoxicity, UNBS3157 has a maximum tolerated dose 3-4 times higher and does not cause hematotoxicity in mice at effective antitumor doses. In vivo models, including (i) L1210 mouse leukemia, (ii) MXT-HI mouse mammary adenocarcinoma, and (iii) human A549 non-small cell lung carcinoma and BxPC3 pancreatic cancer orthotopic models, demonstrate superior efficacy of UNBS3157 compared to Amonafide. |
别名 | UNBS 3157, UNBS3157, UNBS-3157 |
分子量 | 471.72 |
分子式 | C19H17Cl3N4O4 |
CAS No. | 868962-26-9 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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