Topoisomerase I inhibitor 8

Name: Topoisomerase I inhibitor 8
Brand: MedChemExpress
SKU: HY-148058
Rating: 4.5 (0 reviews)

Cat. No.: HY-148058 Pureza: 99.87%: Ficha de datos
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Topoisomerase I inhibitor 8 is a potent topoisomerase I inhibitor. Topoisomerase I inhibitor 8 is a hexacyclic analogue of camptothecin, and displays cytotoxic effect against tumor cells.

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Topoisomerase I inhibitor 8 Estructura química

No. CAS : 210346-40-0

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
50 mg	Obtener un presupuesto
100 mg	Obtener un presupuesto

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Topoisomerase Topo I Topo II DNA gyrase

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Descripciòn

Topoisomerase I inhibitor 8 is a potent topoisomerase I inhibitor. Topoisomerase I inhibitor 8 is a hexacyclic analogue of camptothecin, and displays cytotoxic effect against tumor cells^[1].

IC₅₀ & Target

Topoisomerase I

Cellular Effect

Cell Line	Type	Value	Description	References
HOC-21 cell line	IC₅₀	2.06 ng/mL Compound: 57	In vitro antitumor activity against HOC-21 (human ovarian cancer) cells. In vitro antitumor activity against HOC-21 (human ovarian cancer) cells.	[PMID: 9632364]
P388	IC₅₀	0.22 ng/mL Compound: 57	In vitro antitumor activity against P388 (murine leukemia) cells. In vitro antitumor activity against P388 (murine leukemia) cells.	[PMID: 9632364]
QG-56	IC₅₀	0.17 ng/mL Compound: 57	In vitro antitumor activity against QG-56 (human lung cancer) cells. In vitro antitumor activity against QG-56 (human lung cancer) cells.	[PMID: 9632364]

In Vitro

Topoisomerase I inhibitor 8 (compound 57) shows antitumor activities against three cell line cultures with IC₅₀s of 0.22 ng/mL (P388), 2.06 ng/mL (HOC-21), 0.17 ng/mL (QG-56), respectively^[1].
Topoisomerase I inhibitor 8 results the change in DNA from the supercoiled form to the relaxed form in the presence of topoisomerase I, shows stronger effective than SN-38 (HY-13704), with IC₅₀ of compound/IC₅₀ of SN-38=0.51^[1].

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

Peso molecular

420.43

Fòrmula

C₂₄H₂₁FN₂O₄

No. CAS

210346-40-0

Appearance

Solid

Color

Light yellow to brown

SMILES

CC1=C(F)C=C2C3=C1CCCC3=C4C(C(N5C4)=CC([C@](CC)(O)C(OC6)=O)=C6C5=O)=N2

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (118.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3785 mL	11.8926 mL	23.7852 mL
5 mM	0.4757 mL	2.3785 mL	4.7570 mL
10 mM	0.2379 mL	1.1893 mL	2.3785 mL

View the Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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

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Working solution concentration: mg/mL

Pureza y Documentación

Purity: 99.87%

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Ficha de datos (277 KB) SDS (251 KB)

COA (257 KB) HNMR (437 KB) RP-HPLC (260 KB) LCMS (94 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Sugimori M, et al. Synthesis and antitumor activity of ring A- and F-modified hexacyclic camptothecin analogues. J Med Chem. 1998 Jun 18;41(13):2308-18. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3785 mL	11.8926 mL	23.7852 mL	59.4629 mL
	5 mM	0.4757 mL	2.3785 mL	4.7570 mL	11.8926 mL
	10 mM	0.2379 mL	1.1893 mL	2.3785 mL	5.9463 mL
	15 mM	0.1586 mL	0.7928 mL	1.5857 mL	3.9642 mL
	20 mM	0.1189 mL	0.5946 mL	1.1893 mL	2.9731 mL
	25 mM	0.0951 mL	0.4757 mL	0.9514 mL	2.3785 mL
	30 mM	0.0793 mL	0.3964 mL	0.7928 mL	1.9821 mL
	40 mM	0.0595 mL	0.2973 mL	0.5946 mL	1.4866 mL
	50 mM	0.0476 mL	0.2379 mL	0.4757 mL	1.1893 mL
	60 mM	0.0396 mL	0.1982 mL	0.3964 mL	0.9910 mL
	80 mM	0.0297 mL	0.1487 mL	0.2973 mL	0.7433 mL
	100 mM	0.0238 mL	0.1189 mL	0.2379 mL	0.5946 mL