所有图片(3)
别名:
(S)-4,11-二乙基-3,4,12,14-四氢-4-羟基-3,14-二氧代-1H-吡喃并[3′,4′:6,7]中氮茚并[1,2-b]喹啉-9-基酯, CPT-11, [1,4′-联吡啶]-1′-羧酸
经验公式（希尔记法）:
C33H38N4O6 · HCl
推荐产品
生物来源
plant (Fructus camptothecae)
检测方案
≥97% (HPLC)
形式
powder
溶解性
DMSO: 50 mg/mL
储存温度
2-8°C
SMILES字符串
Cl.CCc1c2CN3C(=O)C4=C(C=C3c2nc5ccc(OC(=O)N6CCC(CC6)N7CCCCC7)cc15)[C@@](O)(CC)C(=O)OC4
InChI
1S/C33H38N4O6.ClH/c1-3-22-23-16-21(43-32(40)36-14-10-20(11-15-36)35-12-6-5-7-13-35)8-9-27(23)34-29-24(22)18-37-28(29)17-26-25(30(37)38)19-42-31(39)33(26,41)4-2;/h8-9,16-17,20,41H,3-7,10-15,18-19H2,1-2H3;1H/t33-;/m0./s1
InChI key
GURKHSYORGJETM-WAQYZQTGSA-N
基因信息
human ... TOP1(7150)
应用
盐酸伊立替康用于：:
- 与5-氟尿嘧啶联合使用，在MDA-MB-231乳腺癌细胞中筛选生长抑制功能。
- 在高级别阑尾癌（HGA）和低级别阑尾癌（LGA）中筛选化学敏感性。
- 作为化学治疗剂，与热休克蛋白抑制剂（HPSC1）联合使用，研究对HT29结肠癌细胞的细胞毒性。
生化/生理作用
抗癌药伊立替康是一种前药，在组织羧酸酯酶作用下转化为7-乙基-10-羟基喜树碱（SN-38）——一种有效的DNA拓扑异构酶I抑制剂。通过UDP葡萄糖醛酸转移酶1A1（UGT1A1）的葡萄糖醛酸化作用，可终止该药的作用。该药物能增强组织对辐射损伤的敏感性，因此可用于肿瘤的放射治疗。
抗癌药伊立替康是一种前药，在组织羧酸酯酶作用下转化为7-乙基-10-羟基喜树碱（SN-38）——一种有效的DNA拓扑异构酶I抑制剂。通过UDP葡萄糖醛酸转移酶的葡萄糖醛酸化作用，可终止该药的作用。
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Votanopoulos K, et al.
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Francesco Crea et al.
Molecular cancer therapeutics, 8(7), 1964-1973 (2009-06-18)
Irinotecan is a topoisomerase-I (Top-I) inhibitor used for the treatment of colorectal cancer. DNA demethylating agents, including 5-azacytidine (5-aza), display synergistic antitumor activity with several chemotherapy drugs. 5-Aza may enhance irinotecan cytotoxicity by at least one of the following mechanisms:
Re-examining HSPC1 inhibitors
Lee S, et al.
Cell Stress & Chaperones, 22(2), 293-306 (2017)
Hiroshi Kimura et al.
Journal of laboratory automation, 20(3), 265-273 (2014-11-12)
Testing of drug effects and cytotoxicity by using cultured cells has been widely performed as an alternative to animal testing. However, the estimation of pharmacokinetics by conventional cell-based assay methods is difficult because of the inability to evaluate multiorgan effects.
T C Chang et al.
Cancer chemotherapy and pharmacology, 75(3), 579-586 (2015-01-13)
To define the dose-limiting toxicity (DLT), maximum tolerated dose (MTD) and pharmacokinetics (PK) of PEP02, a novel liposome-encapsulated irinotecan, in patients with advanced refractory solid tumors. Patients were enrolled in cohorts of one to three to receive escalating dose of
商品
喹诺酮类药物是一类重要的抗生素，它们通过抑制拓扑异构酶来干扰DNA合成，最常见的是拓扑异构酶II（DNA旋转酶），它是一种参与DNA复制的酶。
Quinolones are a key group of antibiotics that interfere with DNA synthesis by inhibiting topoisomerase, most frequently topoisomerase II (DNA gyrase), an enzyme involved in DNA replication.
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