上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
Mitoxantrone diacetate (Synonyms: NSC 299195; Mitozantrone diacetate)
Mitoxantrone diacetate 是一种有效的拓扑异构酶II (topoisomerase II) 抑制剂。Mitoxantrone diacetate 也可抑制蛋白激酶 C (PKC)，其 IC50 值为 8.5 μM。Mitoxantrone diacetate 诱导 B- 慢性淋巴细胞白血病 (B-CLL) 细胞凋亡 (apoptosis)。Mitoxantrone diacetate 具有抗肿瘤活性。
Mitoxantrone diacetate Chemical Structure
CAS No. : 70711-41-0
| 规格 |
|
是否有货 |
|
| 100 mg |
|
询价 |
|
| 250 mg |
|
询价 |
|
| 500 mg |
|
询价 |
|
* Please select Quantity before adding items.
Mitoxantrone diacetate 的其他形式现货产品:
Mitoxantrone Mitoxantrone dihydrochloride
| 生物活性 |
Mitoxantrone diacetate is a potent topoisomerase II inhibitor. Mitoxantrone diacetate also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone diacetate induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone diacetate shows antitumor activity[1][2][3][4].
|
| IC50 & Target |
|
Topoisomerase II
|
PKC
8.5 μM (IC50)
|
|
体外研究
(In Vitro) |
Mitoxantrone diacetate inhibits PKC in a competitive manner with respect to histone H1, and its Ki value is 6.3 μM and in a non-competitive manner with respect to phosphatidylserine and ATP[1].
Mitoxantrone diacetate (0.5 μg/mL, 48 h) induces a decrease in B-CLL cells. Mitoxantrone diacetate induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), demonstrating that the cytotoxic effect of Mitoxantrone diacetate is due to induction of apoptosis[2].
Mitoxantrone diacetate shows cytotoxicity to human breast carcinoma cell lines MDA-MB-231 and MCF-7 with IC50 values of 18 and 196 nM, respectively[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
|
体内研究
(In Vivo) |
Mitoxantrone diacetate (IP, 1.6 mg/kg/day; as a free base) produces a statistically significant number of 60-day survivors (curative effect) in mice with IP implanted L1210 leukemia[4].
In SC implanted Lewis lung carcinoma, Mitoxantrone diacetate and ADM administered IV also shows effective antitumor activities and produces a 60% and a 45% ILS, respectively[4].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
|
| 分子量 |
|
| Formula |
|
| 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.
|
| 参考文献 |
-
[1]. Takeuchi N, et al. Inhibitory effect of mitoxantrone on activity of protein kinase C and growth of HL60 cells. J Biochem. 1992 Dec;112(6):762-7.
[2]. Bellosillo B, et al. Mitoxantrone, a topoisomerase II inhibitor, induces apoptosis of B-chronic lymphocytic leukaemia cells. Br J Haematol. 1998 Jan;100(1):142-6.
[3]. Vibet S, et al. Differential subcellular distribution of mitoxantrone in relation to chemosensitization in two human breast cancer cell lines. Drug Metab Dispos. 2007 May;35(5):822-8.
[4]. Fujimoto S, et al. Antitumor activity of mitoxantrone against murine experimental tumors: comparative analysis against various antitumor antibiotics. Cancer Chemother Pharmacol. 1982;8(2):157-62.
|
所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务
