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经验公式(希尔记法):
C33H38N4O6 · HCl
化学文摘社编号:
分子量:
623.14
UNSPSC Code:
12352204
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
伊立替康 盐酸盐, topoisomerase inhibitor
SMILES string
Cl.CCc1c2CN3C(=O)C4=C(C=C3c2nc5ccc(OC(=O)N6CCC(CC6)N7CCCCC7)cc15)[C@@](O)(CC)C(=O)OC4
InChI key
GURKHSYORGJETM-WAQYZQTGSA-N
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
biological source
plant (Fructus camptothecae)
assay
≥97% (HPLC)
form
powder
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
Gene Information
human ... TOP1(7150)
Application
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。
Biochem/physiol Actions
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。
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。
Appendiceal Cancer Patient-Specific Tumor Organoid Model for Predicting Chemotherapy Efficacy Prior to Initiation of Treatment: A Feasibility Study
Votanopoulos K, et al.
Annals of Surgical Oncology, 26(1), 139-147 (2019)
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
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.
商品
Explore how antibiotics, particularly quinolones, inhibit nucleic acid synthesis by targeting topoisomerases, crucial for DNA replication processes.
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。
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