1. Cell Cycle/DNA Damage
  2. Topoisomerase
  3. Topovale

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

Topovale Chemical Structure

CAS No. : 500214-53-9

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  • 生物活性

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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
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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

质量   浓度   体积   分子量 *
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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)
× = ×
C1   V1   C2   V2
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.

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产品名称:
Topovale
目录号:
HY-118942
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