製品番号: HY-18351

Indotecan

(別名: LMP-400; NSC-724998)

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Based on 1 Customer Validation

Indotecan (LMP-400), an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC₅₀s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 98.0%
CAS 番号: 915303-09-2
分子式: C₂₆H₂₆N₂O₇
分子量:478.49

保管条件:

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Indotecan 構造式

CAS 番号: 915303-09-2

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

Topoisomerase I

Topoisomerase アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
DU-145	GI₅₀	0.155 μM Compound: 6, indotecan	Antiproliferative activity against human DU145 cells by SRB assay Antiproliferative activity against human DU145 cells by SRB assay	[PMID: 21710981]
DU-145	GI₅₀	0.155 μM Compound: 6; MP400; NSC 724998	Antiproliferative activity in human DU145 cells assessed as cell growth inhibition after 48 hrs by SRB assay Antiproliferative activity in human DU145 cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27097152]
DU-145	GI₅₀	0.155 μM Compound: 11	Cytotoxicity against human DU145 cell line Cytotoxicity against human DU145 cell line	[PMID: 17034134]
DU-145	GI₅₀	0.155 μM Compound: 5	Cytotoxicity against human DU145 cells Cytotoxicity against human DU145 cells	[PMID: 20630766]
HCT-116	GI₅₀	1.15 μM Compound: 6, indotecan	Antiproliferative activity against human HCT116 cells by SRB assay Antiproliferative activity against human HCT116 cells by SRB assay	[PMID: 21710981]
HCT-116	GI₅₀	1.15 μM Compound: 6; MP400; NSC 724998	Antiproliferative activity in human HCT116 cells assessed as cell growth inhibition after 48 hrs by SRB assay Antiproliferative activity in human HCT116 cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27097152]
HCT-116	GI₅₀	1.15 μM Compound: 11	Cytotoxicity against human HCT116 cell line Cytotoxicity against human HCT116 cell line	[PMID: 17034134]
HCT-116	GI₅₀	1.15 μM Compound: 5	Cytotoxicity against human HCT116 cells Cytotoxicity against human HCT116 cells	[PMID: 20630766]
HOP-62	GI₅₀	1.78 μM Compound: 6, indotecan	Antiproliferative activity against human HOP62 cells by SRB assay Antiproliferative activity against human HOP62 cells by SRB assay	[PMID: 21710981]
HOP-62	GI₅₀	1.78 μM Compound: 6; MP400; NSC 724998	Antiproliferative activity in human HOP62 cells assessed as cell growth inhibition after 48 hrs by SRB assay Antiproliferative activity in human HOP62 cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27097152]
HOP-62	GI₅₀	1.78 μM Compound: 11	Cytotoxicity against human HOP62 cell line Cytotoxicity against human HOP62 cell line	[PMID: 17034134]
HOP-62	GI₅₀	1.78 μM Compound: 5	Cytotoxicity against human HOP62 cells Cytotoxicity against human HOP62 cells	[PMID: 20630766]
MCF7	GI₅₀	0.37 μM Compound: 6, indotecan	Antiproliferative activity against human MCF7 cells by SRB assay Antiproliferative activity against human MCF7 cells by SRB assay	[PMID: 21710981]
MCF7	GI₅₀	0.37 μM Compound: 5	Cytotoxicity against human MCF7 cells Cytotoxicity against human MCF7 cells	[PMID: 20630766]
MCF7	GI₅₀	0.374 μM Compound: 6; MP400; NSC 724998	Antiproliferative activity in human MCF7 cells assessed as cell growth inhibition after 48 hrs by SRB assay Antiproliferative activity in human MCF7 cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27097152]
MDA-MB-435	GI₅₀	67.6 μM Compound: 11	Cytotoxicity against human MDA-MB-435 cell line Cytotoxicity against human MDA-MB-435 cell line	[PMID: 17034134]
OVCAR-3	GI₅₀	74.1 μM Compound: 6, indotecan	Antiproliferative activity against human OVCAR3 cells by SRB assay Antiproliferative activity against human OVCAR3 cells by SRB assay	[PMID: 21710981]
OVCAR-3	GI₅₀	74.1 μM Compound: 11	Cytotoxicity against human OVCAR-3 cell line Cytotoxicity against human OVCAR-3 cell line	[PMID: 17034134]
OVCAR-3	GI₅₀	74.1 μM Compound: 5	Cytotoxicity against human OVCAR-3 cells Cytotoxicity against human OVCAR-3 cells	[PMID: 20630766]
SF-539	GI₅₀	0.04 μM Compound: 6, indotecan	Antiproliferative activity against human SF539 cells by SRB assay Antiproliferative activity against human SF539 cells by SRB assay	[PMID: 21710981]
SF-539	GI₅₀	0.04 μM Compound: 6; MP400; NSC 724998	Antiproliferative activity in human SF539 cells assessed as cell growth inhibition after 48 hrs by SRB assay Antiproliferative activity in human SF539 cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27097152]
SF-539	GI₅₀	0.04 μM Compound: 11	Cytotoxicity against human SF539 cell line Cytotoxicity against human SF539 cell line	[PMID: 17034134]
SF-539	GI₅₀	0.04 μM Compound: 5	Cytotoxicity against human SF539 cells Cytotoxicity against human SF539 cells	[PMID: 20630766]
SN12C	GI₅₀	0.813 μM Compound: 6, indotecan	Antiproliferative activity against human SN12C cells by SRB assay Antiproliferative activity against human SN12C cells by SRB assay	[PMID: 21710981]
SN12C	GI₅₀	0.813 μM Compound: 6; MP400; NSC 724998	Antiproliferative activity in human SN12C cells assessed as cell growth inhibition after 48 hrs by SRB assay Antiproliferative activity in human SN12C cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27097152]
SN12C	GI₅₀	0.813 μM Compound: 11	Cytotoxicity against human SN12C cell line Cytotoxicity against human SN12C cell line	[PMID: 17034134]
SN12C	GI₅₀	0.813 μM Compound: 5	Cytotoxicity against human SN12C cells Cytotoxicity against human SN12C cells	[PMID: 20630766]
UACC-62	GI₅₀	0.03 μM Compound: 6, indotecan	Antiproliferative activity against human UACC62 cells by SRB assay Antiproliferative activity against human UACC62 cells by SRB assay	[PMID: 21710981]
UACC-62	GI₅₀	0.03 μM Compound: 6; MP400; NSC 724998	Antiproliferative activity in human UACC62 cells assessed as cell growth inhibition after 48 hrs by SRB assay Antiproliferative activity in human UACC62 cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27097152]
UACC-62	GI₅₀	0.03 μM Compound: 11	Cytotoxicity against human UACC62 cell line Cytotoxicity against human UACC62 cell line	[PMID: 17034134]
UACC-62	GI₅₀	0.03 μM Compound: 5	Cytotoxicity against human UACC62 cells Cytotoxicity against human UACC62 cells	[PMID: 20630766]

体外実験

Indotecan (48 h) inhibits the proliferation of L. infantum promastigotes, ex vivo-infected splenocytes, and uninfected splenocytes, with IC₅₀s of 0.10 μM, 0.10 μM, and 57.16 μM, respectively^[2].
Indotecan (1.1-90 μM; 30 min) induces TopI-DNA complexes and inhibits DNA synthesis in L. infantum cultures^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Indotecan (2.5 mg/kg; i.p. every 2 d for 15 d) depletes the parasitic burden in the spleen and liver of visceral leishmaniasis mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female BALB/c mice (4-6 weeks) were infected with metacyclic parasites intravenously through the tail vein^[2]
Dosage:

2.5 mg/kg body weight per injection
Administration:

Intraperitoneally every 2 days for 15 days (total, eight doses)
Result:

A drastic reduction of the number of transforming amastigotes recovered from the target organs of drug-treated animals was observed.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 915303-09-2
性状 Solid
分子量 478.49
分子式 C₂₆H₂₆N₂O₇
Color White to gray
SMILES

O=C1C2=CC(OC)=C(OC)C=C2C3=C(C(C=C(OCO4)C4=C5)=C5C3=O)N1CCCN6CCOCC6
別名

LMP-400; NSC-724998
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶剤 & 溶解度

体外:

DMSO : 1.23 mg/mL (2.57 mM; ultrasonic and adjust pH to 6 with 1 M HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0899 mL

10.4495 mL

20.8991 mL

5 mM

---

10 mM

---

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 0.12 mg/mL (0.25 mM); Clear solution

This protocol yields a clear solution of ≥ 0.12 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (1.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.12 mg/mL (0.25 mM); Clear solution

This protocol yields a clear solution of ≥ 0.12 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (1.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (279 KB)
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- Portuguese - PT (252 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Balaña-Fouce R, et, al. Indotecan (LMP400) and AM13-55: two novel indenoisoquinolines show potential for treating visceral leishmaniasis. Antimicrob Agents Chemother. 2012 Oct;56(10):5264-70. [Content Brief]

[2]. Seol Y, et, al. Single-Molecule Supercoil Relaxation Assay as a Screening Tool to Determine the Mechanism and Efficacy of Human Topoisomerase IB Inhibitors. Mol Cancer Ther. 2015 Nov;14(11):2552-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0899 mL	10.4495 mL	20.8991 mL	52.2477 mL

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Indotecan

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