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商品详情
名称
Gimatecan, DNA 拓扑异构酶 I 抑制剂
分子类型
小分子
别名
吉马替康
英文别名
1H-Pyrano(3',4':6,7)indolizino(1,2-b)quinoline-11-carboxaldehyde, 4-ethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-, 11-(O-(1,1-dimethylethyl)oxime), (C(E),4S)- | NSC-18169 | NCGC00253588-01 | 1H-Pyrano[3',4':6,7]indolizino[1,2-b]quinoline-11-carboxaldeh
英文名称
Gimatecan
货号
G646499-5mg
包装规格
5mg
浓度
≥99%
储存温度
-20°C储存
运输条件
超低温冰袋运输
产品介绍
Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity In Vitro Gimatecan (3 to 300 ng/mL) significantly inhibits the growth of human bladder cancer models (HT1376 and MCR), thus reflecting antiproliferative potency. Gimatecan causes a persistent S-phase arrest At 0.003 µg/mL and the number of S-phase cells increased after treatment with a higher concentration (0.03 µg/mL). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: HT1376 cells harbor a p53 mutation; MCR cells harbor two p53 mutations: one in exon 4 (CGC→CCC) and one in exon 9 (CAG→TAG) Concentration: 3 to 300 ng/mL Incubation Time: 1, 6, and 24 hours Result: IC 50 s of 90±3 and 9.0±0.4 ng/mL for MCR and HT1376 cells after treatment for 1 hours. IC 50 s of 5.0±0.2 and 2.8±0.1 ng/mL for MCR and HT1376 cells after treatment for 24 hours. The growth-inhibitory effect was dose-dependent and time-dependent. HT1376 cells were more sensitive than MCR cells at least following a short-term exposure. In Vivo Gimatecan (2 mg/kg; treatment per os, every fourth day for four times) is effective for inhibiting tumor growth . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Athymic Swiss nude mice bearing HT1376 model Dosage: 2 mg/kg Administration: Treatment per os, every fourth day for four times Result: Caused a marked tumor growth inhibition during treatment. Form:Solid IC50& Target:Topoisomerase I
生化机理
Gimatecan (ST1481) 是一种强效的拓扑异构酶 I 抑制剂。Gimatecan 是一种可口服的喜树碱类似物，具有抗肿瘤活性。
CAS号
292618-32-7
分子式
C25H25N3O5
分子量
447.48 g/mol
EC号
695-730-5
PubChem编号
9577124
Isomeric SMILES
CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=C(C5=CC=CC=C5N=C4C3=C2)/C=N/OC(C)(C)C)O
IIUPAC Name
(19S)-19-ethyl-19-hydroxy-10-[(E)-(2-methylpropan-2-yl)oxyiminomethyl]-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4,6,8,10,15(20)-heptaene-14,18-dione
INCHI
1S/C25H25N3O5/c1-5-25(31)18-10-20-21-16(12-28(20)22(29)17(18)13-32-23(25)30)15(11-26-33-24(2,3)4)14-8-6-7-9-19(14)27-21/h6-11,31H,5,12-13H2,1-4H3/b26-11+/t25-/m0/s1
InChi Key
UIVFUQKYVFCEKJ-OPTOVBNMSA-N
Smiles
CCC1(C2=C(COC1=O)C(=O)N3CC4=C(C5=CC=CC=C5N=C4C3=C2)C=NOC(C)(C)C)O
PubChem CID
9577124
关联CAS
292618-32-7,292620-90-7
MeSH Entry Terms
7-t-butoxyiminomethyl-camptothecin;7-t-butoxyiminomethylcamptothecin;Gimatecan;LBQ707;ST 1481;ST1481
溶解性
DMSO : 33.33 mg/mL (74.48 mM; ultrasonic and warming and adjust pH to 10 with NaOH and heat to 60°C)
氢键供体数Hydrogen Bond Donor Count
1
氢键受体数Hydrogen Bond Acceptor Count
7
可旋转键计数Rotatable Bond Count
4
精确质量Exact Mass
447.179 Da
单同位素质量Monoisotopic Mass
447.179 Da
拓扑极表面积Topological Polar Surface Area
101.000 Ų
重原子数Heavy Atom Count
33
形式电荷Formal Charge
0
复杂度Complexity
948.000
同位素原子数Isotope Atom Count
0
共价键合单元计数Covalently-Bonded Unit Count
1
XLogP3
2.000
ALogP
2
作用类型
抑制剂
作用机制
DNA 拓扑异构酶 I 抑制剂
危险属性
「暂无危险属性」
上下游信息
「暂无上下游信息」
技术文档
「暂无技术文档」
相关文章
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Gimatecan, DNA 拓扑异构酶 I 抑制剂 5mg
品牌：阿拉丁
货号：G646499-5mg
级别： ≥99%
货期：30天
已售 502 件
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