Simmitecan hydrochloride

Names

[ Name ]:
Simmitecan hydrochloride

[Synonym ]:
(4S)-10-Allyl-4-ethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl 1,4'-bipiperidine-1'-carboxylate hydrochloride (1:1)
[1,4'-Bipiperidine]-1'-carboxylic acid, (4S)-4-ethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-10-(2-propen-1-yl)-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl ester, hydrochloride (1:1)
Simmitecan hydrochloride
Simmitecan hydrochloride salt
T4H02O147G

Biological Activity

[Description]:

Simmitecan hydrochloride, a 9-substituted lipophilic Camptothecin (HY-16560) derivative, is a potent topoisomerase I inhibitor. Simmitecan hydrochloride is an anticancer agent[1][2].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase

Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450

[In Vitro]

Simmitecan hydrochloride 对 CYP2D6 有弱抑制作用 (IC50: 32.9 μM)，对 CYP3A4 有中等抑制作用 (IC50: 8.95 μM)[2]。

[In Vivo]

Simmitecan hydrochloride (3.75、7.5 和 15 mg/kg, SD 大鼠, 静脉推注) 显示平均消除半衰期 t1/2 约为 1.4 小时[2]。

[References]

[1]. Rini B, et al. A phase I/II study of lenalidomide in combination with sunitinib in patients with advanced or metastatic renal cell carcinoma. Ann Oncol. 2014 Sep;25(9):1794-1799.

[2]. Hu ZY, et al. Pharmacokinetic evaluation of the anticancer prodrug simmitecan in different experimental animals. Acta Pharmacol Sin. 2013 Nov;34(11):1437-48.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₄H₃₉ClN₄O₆

[ Molecular Weight ]:
635.150

[ Exact Mass ]:
634.255798

Related Compounds

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