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Merck
CN

T2705

拓扑替康 盐酸盐 水合物

≥98% (HPLC and enzymatic), powder, topoisomerase I inhibitor

别名:

9-[（二甲基氨基）甲基]-10-羟基-（20S）-喜树碱 盐酸盐 水合物, NSC-609669 盐酸盐 水合物, SKF-104864A 盐酸盐 水合物, 拓扑替康 盐酸盐 水合物

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关于此项目

经验公式（希尔记法）:
C23H23N3O5 · xHCl · yH2O
化学文摘社编号:
123948-87-8
分子量:
421.45 (anhydrous free base basis)
UNSPSC Code:
12352200
PubChem Substance ID:
329826724
NACRES:
NA.77
MDL number:
MFCD00870670
Assay:
≥98% (HPLC and enzymatic)
Form:
powder
Quality level:
100
Storage condition:
desiccated
protect from light

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产品名称

拓扑替康 盐酸盐 水合物, ≥98% (HPLC and enzymatic)

SMILES string

[n]21c(cc5c([c]2=O)COC(=O)[C@]5(O)CC)c3nc4c(cc3C1)c(c(cc4)O)CN(C)C

InChI

1S/C23H23N3O5/c1-4-23(30)16-8-18-20-12(9-26(18)21(28)15(16)11-31-22(23)29)7-13-14(10-25(2)3)19(27)6-5-17(13)24-20/h5-8,27,30H,4,9-11H2,1-3H3/t23-/m0/s1

InChI key

UCFGDBYHRUNTLO-QHCPKHFHSA-N

assay

≥98% (HPLC and enzymatic)

form

powder

storage condition

desiccated
protect from light

color

yellow

solubility

DMSO: ≥20 mg/mL

originator

GlaxoSmithKline

storage temp.

−20°C

Quality Level

100

Gene Information

human ... TOP1MT(116447)

相关类别

Application

拓扑替康作为阳性对照，已被用作低氧条件下人神经胶质瘤细胞中HIF-1α 和VEGF抑制剂的鉴定和分析1。它也被用于 体外 PA317细胞的凋亡检测2。

Biochem/physiol Actions

拓扑替康是一种拓扑异构酶I抑制剂和凋亡诱导剂。它是一种有效的抗肿瘤药。

Features and Benefits

该化合物由GlaxoSmithKline开发。要浏览其他药物开发化合物和批准的药物/候选药物列表，单击此处。
这种化合物是ADME毒性和凋亡研究的特色产品。发现更多有关ADME毒性 和 凋亡 的特色产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。

Preparation Note

本品可溶于水，但浓度尚未确定。但多条来源表明，这种化学品在水中的溶解度大于 1 mg/mL。
水合盐酸拓扑替康可溶于DMSO，溶解浓度大于等于20 mg/ml。

pictograms

Health hazard
GHS08

signalword

Danger

Hazard Classifications

Muta. 1B - Repr. 2

存储类别

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

涉药品监管产品
此项目有

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000513908
0000513907
0000513908
0000513907
0000314301

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Ian F King et al.
Nature, 501(7465), 58-62 (2013-09-03)
Topoisomerases are expressed throughout the developing and adult brain and are mutated in some individuals with autism spectrum disorder (ASD). However, how topoisomerases are mechanistically connected to ASD is unknown. Here we find that topotecan, a topoisomerase 1 (TOP1) inhibitor
Andrei Molotkov et al.
Pharmaceutics, 13(3) (2021-04-04)
Glioblastoma (GBM) is the most common primary adult brain malignancy with an extremely poor prognosis and a median survival of fewer than two years. A key reason for this high mortality is that the blood-brain barrier (BBB) significantly restricts systemically
Iben Kümler et al.
Breast cancer research and treatment, 138(2), 347-358 (2013-03-21)
Following treatment with anthracyclines and taxanes, few established options exist for the treatment of metastatic breast cancer (MBC). Although the topoisomerase 1 inhibitors irinotecan, etirinotecan, and topotecan have been used in clinical trials on MBC, the drugs have never been
Jerec W Ricci et al.
Molecular cancer therapeutics, 15(12), 2853-2862 (2016-09-28)
Chemotherapeutic resistance remains a challenge in the treatment of ovarian carcinoma, especially in recurrent disease. Despite the fact that most patients with newly diagnosed tumors attain complete remission following cytoreductive surgery and chemotherapy, ovarian carcinoma has a recurrence rate that
Kaleem Ashraf et al.
Pediatric blood & cancer, 60(10), 1636-1641 (2013-05-08)
Reports of responses and toxicities of salvage therapies for relapsed neuroblastoma are rare and often confounded by effects of additional treatments. Our objective was to describe the outcomes and toxicities for a topotecan and cyclophosphamide (TOPO/CTX) regimen for first relapse
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