Campathecin 纯度:98.26% 500mg

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Campathecin 纯度:98.26% 500mg

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Campathecin 是有效的 DNA拓扑异构酶 I 抑制剂，IC₅₀ 值为 679 nM。

Description

Campathecin is a potent DNA enzyme topoisomerase I inhibitor, with an IC₅₀ of 679 nM.

IC₅₀ & Target

Topoisomerase I

679 nM (IC₅₀)

In Vitro

[³H]BrCPT labeling of topoisomerase I is enhanced greatly by the presence of DNA; very little labeling of isolated topoisomerase I or isolated DNA occurrs. Even in the presence of DNA, [³H]BrCPT labeling of topoisomerase I is inhibited by camptothecin, suggesting that both CPT and BrCPT bind to the same site on the DNA-topoisomerase I binary complex^[1]. With increasing concentrations of camptothecin, closed circular pRR322 DNA (form I) is converted to nicked circular DNA (form 11). This apparent nicking activitv of camptothecin required DNA topoisomerase I^[2].

Solvent & Solubility

In Vitro:

DMSO : 20.66 mg/mL (59.31 mM; Need warming)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8707 mL	14.3534 mL	28.7068 mL
5 mM	0.5741 mL	2.8707 mL	5.7414 mL
10 mM	0.2871 mL	1.4353 mL	2.8707 mL

* Please refer to the solubility information to select the appropriate solvent.

References

[1]. Hertzberg RP, et al. Irreversible trapping of the DNA-topoisomerase I covalent complex. Affinity labeling of the camptothecin binding site. J Biol Chem. 1990 Nov 5;265(31):19287-95.

[2]. Hsiang YH, et al. Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I. J Biol Chem. 1985 Nov 25;260(27):14873-8.

[3]. Luzzio MJ, et al. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.

Kinase Assay ^[1]	Each reaction mixture (200 μL, total volume) contained 2 μg of supercoiled pDPT2789 DNA (2.4 nM plasmid concentration), 50 mM Tris-HCl, pH 7.5, 120 mM KCl, 10 mM MgCl₂, 0.5 mM EDTA, 0.05% dimethyl sulfoxide, 1% methanol, 100 μg/mL BSA, 4.3 ng of calf thymus topoisomerase I (0.26 nM), and a CPT derivative. The reaction mixture is incubated at 37°C, and at the indicated times 20-μL aliquots are removed and terminated by the addition of 5 μL of SDS/Ficoll stop mix (final concentrations, 0.5% SDS, 2% Ficoll, 0.025% bromphenol blue). The samples are loaded onto a 1% agarose gel and analyzed by electrophoresis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Hertzberg RP, et al. Irreversible trapping of the DNA-topoisomerase I covalent complex. Affinity labeling of the camptothecin binding site. J Biol Chem. 1990 Nov 5;265(31):19287-95. [2]. Hsiang YH, et al. Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I. J Biol Chem. 1985 Nov 25;260(27):14873-8. [3]. Luzzio MJ, et al. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.

Kinase Assay
^[1]

Each reaction mixture (200 μL, total volume) contained 2 μg of supercoiled pDPT2789 DNA (2.4 nM plasmid concentration), 50 mM Tris-HCl, pH 7.5, 120 mM KCl, 10 mM MgCl₂, 0.5 mM EDTA, 0.05% dimethyl sulfoxide, 1% methanol, 100 μg/mL BSA, 4.3 ng of calf thymus topoisomerase I (0.26 nM), and a CPT derivative. The reaction mixture is incubated at 37°C, and at the indicated times 20-μL aliquots are removed and terminated by the addition of 5 μL of SDS/Ficoll stop mix (final concentrations, 0.5% SDS, 2% Ficoll, 0.025% bromphenol blue). The samples are loaded onto a 1% agarose gel and analyzed by electrophoresis.

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

References

[1]. Hertzberg RP, et al. Irreversible trapping of the DNA-topoisomerase I covalent complex. Affinity labeling of the camptothecin binding site. J Biol Chem. 1990 Nov 5;265(31):19287-95.

[2]. Hsiang YH, et al. Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I. J Biol Chem. 1985 Nov 25;260(27):14873-8.

[3]. Luzzio MJ, et al. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.

Molecular Weight	348.35
Formula	C₂₀H₁₆N₂O₄
CAS No.	7689-03-4
SMILES	O=C1C2=C([C@@](O)(CC)C(OC2)=O)C=C(N1C3)C(C3=C4)=NC5=C4C=CC=C5
Storage	4°C, protect from light
Shipping	Room temperature in continental US; may vary elsewhere