计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
避光,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 96 篇同行评审文献引用。
概述
Information
Camptothecin (NSC-100880, CPT, Campathecin, (S)-(+)-Camptothecin) is a specific inhibitor of DNAtopoisomerase I (Topo I)withIC50of 0.68 μM in a cell-free assay. Camptothecin inducesapoptosisin cancer cells via microRNA-125b-mediated mitochondrial pathways
In vitro
Camptothecin, a plant alkaloid orignially isolated from Camptotheca acuminate in 1966. Camptothecin is noted to halt cells during the S phase of mitosis. Camptothecin displays nanomolar potency in cytotoxicity against many human tumor cell lines, including HT29, LOX, SKOV3, and SKVLB, with IC50 values ranging from 37 nM to 48 nM. In combination with TNF, Camptothecin induces apoptosis in primary mouse hepatocytes, with an IC50 value of 13 μM. Camptothecin also abrogated the TNF-induced NF-κB Activation, as well as the expression of TNF-receptor associated factor 2 (TRAF2), X-linked inhibitor of apoptosis protein (X-IAP), and FLICE-inhibitory protein (FLIP). In HCT116 cells, Camptothecin (5 μM) induces proteasome-mediated degradation of mixed lineage leukemia 5 (MLL5) protein, which leads to phosphorylation of p53 at Ser392. Due to the low solubility and adverse effects of Camptothecin, various Camptothecin analogues have been developed, and two of them, topotecan and irinotecan, has been approved by FDA and are used in cancer chemotherapy.
In vivo
Camptothecin (8 mg/kg) displays complete growth inhibition and regression in mice xenografts of various tumors, including colon, lung, breast, stomach, and ovary tumors. In mice, combinations of Camptothecin (50 mg/kg) and TNF (5 and 7 μg/kg), but not Camptothecin alone, induces liver damage.
Cell Data
cell lines：
Concentrations：0.17 nM–10 mM
Incubation Time：48 hours
Powder Purity:≥97%
规格
英文别名
CPT, Campathecin, (S)-(+)-Camptothecin | (4S)-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
规格或纯度
Moligand™, 2mM in DMSO
英文名称
Camptothecin (NSC-100880)
生化机理
喜树碱（NSC-100880，CPT，Campathecin，(S)-(+)-Camptothecin）是 DNA 拓扑异构酶 I（Topo I）的特异性抑制剂，在无细胞试验中的 IC50 值为 0.68 μM。喜树碱通过 microRNA-125b 介导的线粒体途径诱导癌细胞凋亡。第 2 阶段
储存条件
避光,-80℃储存
运输条件
特低温运输
名称和识别符
EC号
616-407-7
分子类型
小分子
Isomeric SMILES
CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=CC5=CC=CC=C5N=C4C3=C2)O
分子量
348.35
Reaxy-Rn
631068
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=631068&ln=
技术文档
高级数据
关联靶点（人）
HNRNPA1
Tchem
异质性核糖核蛋白A1(Heterogeneous nuclear ribonucleoprotein A1)
(1 活性数据)
TOP1
Tclin
DNA拓扑异构酶1(DNA topoisomerase 1)
(10 活性数据)
CHEK1
Tchem
丝氨酸/苏氨酸蛋白激酶 Chk1(Serine/threonine-protein kinase Chk1)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro Water: 71 mg/mL (201.43 mM); DMSO: Insoluble; Ethanol: Insoluble;
比旋光度
+37.0 to +42.0 deg(C=0.4, CHCl3:MeOHl=8:2)
熔点
259-263°C
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
此产品的引用文献
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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