Topovale (Synonyms: ARC 111)

目录号: HY-118942 纯度: 99.94%: Data Sheet SDS COA 产品使用指南
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Topovale (ARC 111) 是一种拓扑异构酶 I 抑制剂。Topovale 是一种抗肿瘤剂，对一系列癌细胞表现出低纳摩尔的细胞毒性。Topovale 在肿瘤细胞中诱导可逆的拓扑异构酶 I (TOP1) 裂解复合物形成。

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Topovale Chemical Structure

CAS No. : 500214-53-9

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规格	价格	是否有货
1 mg	￥1248	In-stock
5 mg	￥2488	In-stock
10 mg	￥3736	In-stock
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100 mg		询价

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Topoisomerase Topo I Topo II

生物活性
纯度 & 产品资料
参考文献

生物活性

Topovale (ARC 111) is a topoisomerase I inhbitor. Topovale is an antitumor agent, and shows low nM cytotoxicity against a panel of cancer cells. Topovale induces reversible topoisomerase I (TOP1) cleavage complexes in tumor cells^[1].

IC₅₀ & Target^[1]

Topoisomerase I

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HCT-116	GI₅₀	0.177 μM Compound: ARC-111	Growth inhibition of human HCT-116 cells by Cell-titer96 assay Growth inhibition of human HCT-116 cells by Cell-titer96 assay	[PMID: 33492141]
KB 3-1	IC₅₀	0.005 μM Compound: 1, ARC-111	Cytotoxicity against human KB3-1 cells after MTT assay Cytotoxicity against human KB3-1 cells after MTT assay	[PMID: 18829334]
KB 3-1	IC₅₀	0.005 μM Compound: 1, ARC-111	Cytotoxicity against human KB3-1 cells after 4 days by MTT method Cytotoxicity against human KB3-1 cells after 4 days by MTT method	[PMID: 19303306]
KB 3-1	IC₅₀	0.005 μM Compound: 1, ARC-111	Cytotoxicity against human KB3-1 cells after 4 days by MTT assay Cytotoxicity against human KB3-1 cells after 4 days by MTT assay	[PMID: 18676151]
KB 3-1	IC₅₀	0.005 μM Compound: 1	Cytotoxicity against human KB3-1 cells by MTT method Cytotoxicity against human KB3-1 cells by MTT method	[PMID: 18771930]
KB 3-1	IC₅₀	0.005 μM Compound: 1, ARC-111	Cytotoxicity against human KB3-1 cells after 4 days after MTT assay Cytotoxicity against human KB3-1 cells after 4 days after MTT assay	[PMID: 19299037]
KB-V1	IC₅₀	0.002 μM Compound: 1, ARC-111	Cytotoxicity against MDR1 overexpressing human KBV1 cells after 4 days by MTT method Cytotoxicity against MDR1 overexpressing human KBV1 cells after 4 days by MTT method	[PMID: 19303306]
KB-V1	IC₅₀	0.005 μM Compound: 1, ARC-111	Cytotoxicity against multidrug resistant human KBV-1 cells overexpressing MDR1 after MTT assay Cytotoxicity against multidrug resistant human KBV-1 cells overexpressing MDR1 after MTT assay	[PMID: 18829334]
KB-V1	IC₅₀	0.005 μM Compound: 1, ARC-111	Cytotoxicity against multidrug resistant human KBV1 cells overexpressing MDR1 after 4 days by MTT assay Cytotoxicity against multidrug resistant human KBV1 cells overexpressing MDR1 after 4 days by MTT assay	[PMID: 19299037]
KB-V1	IC₅₀	0.005 μM Compound: 1	Cytotoxicity against human KBV1 cells by MTT method Cytotoxicity against human KBV1 cells by MTT method	[PMID: 18771930]
KB-V1	IC₅₀	0.015 μM Compound: 1, ARC-111	Cytotoxicity against human multidrug resistant MDR1 overexpressing human KBV1 cells after 4 days by MTT assay Cytotoxicity against human multidrug resistant MDR1 overexpressing human KBV1 cells after 4 days by MTT assay	[PMID: 18676151]
P388	IC₅₀	0.001 μM Compound: 1, ARC-111	Cytotoxicity against mouse P388 cells after MTT assay Cytotoxicity against mouse P388 cells after MTT assay	[PMID: 18829334]
P388	IC₅₀	0.001 μM Compound: 1, ARC-111	Cytotoxicity against mouse P388 cells after 4 days by MTT method Cytotoxicity against mouse P388 cells after 4 days by MTT method	[PMID: 19303306]
P388	IC₅₀	0.001 μM Compound: 1, ARC-111	Cytotoxicity against mouse P388 cells after 4 days by MTT assay Cytotoxicity against mouse P388 cells after 4 days by MTT assay	[PMID: 19299037]
P388	IC₅₀	0.001 μM Compound: 1, ARC-111	Cytotoxicity against mouse P388 cells after 4 days by MTT assay Cytotoxicity against mouse P388 cells after 4 days by MTT assay	[PMID: 18676151]
P388	IC₅₀	0.001 μM Compound: 1	Cytotoxicity against mouse P388 cells by MTT method Cytotoxicity against mouse P388 cells by MTT method	[PMID: 18771930]
P388	IC₅₀	0.23 μM Compound: 1, ARC-111	Cytotoxicity against camptothecin-resistant mouse P388 cells after 4 days by MTT method Cytotoxicity against camptothecin-resistant mouse P388 cells after 4 days by MTT method	[PMID: 19303306]
P388	IC₅₀	0.23 μM Compound: 1, ARC-111	Cytotoxicity against mouse CPT45-resistant topoisomerase 1-deficient P388 cells after 4 days by MTT assay Cytotoxicity against mouse CPT45-resistant topoisomerase 1-deficient P388 cells after 4 days by MTT assay	[PMID: 18676151]
P388	IC₅₀	0.23 μM Compound: 1	Cytotoxicity against camptothecin-resistant mouse P388 cells by MTT method Cytotoxicity against camptothecin-resistant mouse P388 cells by MTT method	[PMID: 18771930]
P388CPT45	IC₅₀	0.23 μM Compound: 1, ARC-111	Cytotoxicity against camptothecin-resistant and TOP1 deficient mouse P388/CPT45 cells after MTT assay Cytotoxicity against camptothecin-resistant and TOP1 deficient mouse P388/CPT45 cells after MTT assay	[PMID: 18829334]
P388CPT45	IC₅₀	0.23 μM Compound: 1, ARC-111	Cytotoxicity against mouse P388/CPT45 cells after 4 days by MTT assay Cytotoxicity against mouse P388/CPT45 cells after 4 days by MTT assay	[PMID: 19299037]
RPMI 8402	IC₅₀	0.002 μM Compound: 1, ARC-111	Cytotoxicity against human RPMI8402 cells after MTT assay Cytotoxicity against human RPMI8402 cells after MTT assay	[PMID: 18829334]
RPMI 8402	IC₅₀	0.002 μM Compound: 1, ARC-111	Cytotoxicity against human RPMI8402 cells after 4 days by MTT method Cytotoxicity against human RPMI8402 cells after 4 days by MTT method	[PMID: 19303306]
RPMI 8402	IC₅₀	0.002 μM Compound: 1, ARC-111	Cytotoxicity against human RPMI8402 cells after 4 days by MTT assay Cytotoxicity against human RPMI8402 cells after 4 days by MTT assay	[PMID: 19299037]
RPMI 8402	IC₅₀	0.002 μM Compound: 1, ARC-111	Cytotoxicity against human RPMI8402 cells after 4 days by MTT assay Cytotoxicity against human RPMI8402 cells after 4 days by MTT assay	[PMID: 18676151]
RPMI 8402	IC₅₀	0.002 μM Compound: 1	Cytotoxicity against human RPMI8402 cells by MTT method Cytotoxicity against human RPMI8402 cells by MTT method	[PMID: 18771930]
RPMI 8402	IC₅₀	0.002 μM Compound: 1	Cytotoxic activity against human lymphoblast tumor cell line RPMI8402 after 4 days of treatment Cytotoxic activity against human lymphoblast tumor cell line RPMI8402 after 4 days of treatment	[PMID: 12747798]
RPMI 8402	IC₅₀	0.9 μM Compound: 3a	Cytotoxicity using camptothecin-resistant variant of RPM18402 (CPT-K5) possessing functional, but mutant TOP-1 Cytotoxicity using camptothecin-resistant variant of RPM18402 (CPT-K5) possessing functional, but mutant TOP-1	[PMID: 12392745]

分子量

421.45

Formula

C₂₃H₂₃N₃O₅

CAS 号

500214-53-9

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 4.03 mg/mL (9.56 mM; ultrasonic and adjust pH to 2 with TFA; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3728 mL	11.8638 mL	23.7276 mL
5 mM	0.4746 mL	2.3728 mL	4.7455 mL
10 mM	---	---	---

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.94%

选择批次：

Data Sheet (599 KB) SDS (251 KB)

COA (289 KB) HNMR (258 KB) RP-HPLC (247 KB) MS (69 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Li TK, et al. Characterization of ARC-111 as a novel topoisomerase I-targeting anticancer drug. Cancer Res. 2003 Dec 1;63(23):8400-7. [Content Brief]

Topovale 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3728 mL	11.8638 mL	23.7276 mL	59.3190 mL
DMSO	5 mM	0.4746 mL	2.3728 mL	4.7455 mL	11.8638 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Topovale500214-53-9ARC 111ARC111ARC-111TopoisomeraseHCT-8colon tumorInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Topovale (Synonyms: ARC 111)