Topotecan HCl 化学構造
分子量: 457.91

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製品説明

  • Compare Topoisomerase Inhibitors
    Topoisomerase製品生物活性の比較
  • 研究分野
  • Topotecan HClのメカニズム

製品の説明

生物活性

製品説明 Topotecan HClは、MCF-7リュック細胞とDU-145リュック細胞のためのトポイソメラーゼI阻害剤で、IC50 がそれぞれ 13 nM と 2 nMです。
ターゲット

MCF-7 Luc cells

DU-145 Luc cells

IC50

13 nM

2 nM [1]

In vitro試験 Stronger drug activity of Topotecan is observed for DU-145 Luc and MCF-7 Luc cells. [1] Topotecan causes cytotoxicity during the course of DNA replication by stabilizing the covalent complex between topoisomerase I and DNA and preventing the religation of enzyme-linked single-strand DNA break. Topotecan stabilizes topoisomerase I/DNA cleavable complexes in radiation-resistant human B-lineage acute lymphoblastic leukemia (ALL) cells, causes rapid apoptotic cell death despite high-level expression of bcl-2 protein, and inhibits ALL cell clonogenic growth in a dose-dependent fashion. [2]
In vivo試験 Animals inoculate s.c. with DU-145 Luc cells and then treated with Topotecan demonstrates significant tumor growth and regression as measured with calipers and luminescent imaging. The correlation coefficient is 0.75 for the control untreated group and 0.93 for the Topotecan-treated group. Similarly, tumor progression and regression are measurable using luminescent imaging for untreated and Topotecan-treated mice inoculated i.p. with MCF-7 Luc cells. [1] Topotecan elicited potent antileukemic activity in severe combined immune-deficiency (SCID) mouse models of human poor prognosis ALL. Topotecan markedly improved event-free survival of SCID mice challenged with otherwise fatal doses of humaln leukemia cells at systemic drug exposure levels. [2] Gliomas preferentially express TRAIL R2 and that treatment with Topotecan significantly up-regulates its expression. [3]
臨床試験 Topotecan plus Pazopanib has entered in a phase II clinical trial in the treatment of ovarian cancer.
特集 Topotecan is a water-soluble derivative of camptothecin.

プロトコル (参考用のみ)

細胞アッセイ:

[1]

細胞株 MCF-7 Luc and DU-145 Luc cells
濃度 0 μg/mL - 0.692 μg/mL
反応時間 96 hours
実験の流れ

Topotecan is dissolved in sterile water to a stock concentration of 1 mg/mL, diluted to 6 μg/mL in cultured medium and then serially diluted 1:4 in opaque, white tissue culture-treated microplates to a final volume of 0.1 mL/well. MCF-7 Luc and DU-145 Luc cells are resuspended in 3×104 cells/mL in DMEM with high glucose containing 10% FBS and 0.5 mg/mL Geneticin; 100 μL of cells are added in each well. Plates are incubated for 4 days at 37 °C in 95% humidity/5% CO2. After incubation, 0.05 mL of 0.1 M HEPES buffer (pH 7.9) containing 50 μg/mL D-luciferin is added to each well. After incubation at room temperature for 10 minutes, the culture microplate is measured in a microplate luminometer and a molecular light imager. Results obtained with the microplate luminometer are calculated using no inhibition control wells without exogenous drug and maximum inhibition control wells containing ATP inhibitor. Results for the molecular light imager are similarly calculated using values obtained with a 5 minutes luminescent imager.

動物実験:

[1]

動物モデル Mice with MCF-7 Luc or DU-145 Luc cells
製剤 PBS
投薬量 0.25 mg/mL
投与方法 Administered via i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Topotecan HCl SDF
分子量 457.91
化学式

C23H23N3O5.HCl

CAS No. 119413-54-6
保管 3年-20℃
2年-80℃in solvent
別名 NSC609699, Nogitecan HCl, SKFS 104864A
溶解度 (25°C) * In vitro DMSO 92 mg/mL (200.91 mM)
Water 92 mg/mL (200.91 mM)
Ethanol <1 mg/mL
In vivo Saline 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 (4S)​-10-​[(dimethylamino)​methyl]​-​4-​ethyl-​4,​9-​dihydroxy-​1H-​pyrano[3',​4':6,​7]​indolizino[1,​2-​b]​quinoline-​3,​14(4H,​12H)​-​dione, hydrochloride (1:1)

文献中の引用 (6)

Frequently Asked Questions

  • Question 1
    I would like get the compound for mice intraperitoneally injection, What would you recommend to improve solubility? What could I use as solvent (%v?) that is nontoxic (unlike Methanol) and could be injected into mice intraperitoneally?

    Answer: Topotecan HCl is generally prepared by Saline for I.P. administration.

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