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

Bisantrene  (Synonyms: 比生群; CL216942)

目錄號(hào): HY-100875 純度: 98.08%
COA 產(chǎn)品使用指南 技術(shù)支持

Bisantrene 是高效的抗癌劑,它通過影響 DNA 插入發(fā)揮細(xì)胞毒性。Bisantrene 靶向真核生物的拓?fù)洚悩?gòu)酶 II。Bisantrene 是 MDR1 的底物。

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Bisantrene Chemical Structure

Bisantrene Chemical Structure

CAS No. : 78186-34-2

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Customer Review

Other Forms of Bisantrene:

查看 Topoisomerase 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Bisantrene is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene targets eukaryotic type II topoisomerases. Bisantrene is a substrate of MDR1[1][2][3][4].

IC50 & Target[1]

Topoisomerase II

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.017 μM
Compound: 1
Compound was tested for potency against human lung A549 cells using sulforhodamine B assay.
Compound was tested for potency against human lung A549 cells using sulforhodamine B assay.
[PMID: 9371238]
RPMI-8226 IC50
0.018 μM
Compound: 1
Compound was tested for potency against human myeloma 8226 cells using MTT assay method.
Compound was tested for potency against human myeloma 8226 cells using MTT assay method.
[PMID: 9371238]
體外研究
(In Vitro)

Bisantrene 促進(jìn) DNase I 在寡嘌呤-寡嘧啶鏈上的切割,并略微降低在交替的嘌呤-嘧啶序列上的切割活性[1]。
Bisantrene 是 [3H]尿苷摻入RNA和 [3H]胸苷摻入 DNA 的抑制劑[2]

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

體內(nèi)研究
(In Vivo)

Bisantrene 是一種抗腫瘤劑,對(duì)多種實(shí)驗(yàn)性腫瘤具有活性,包括 P388 白血病、L1210 白血病、Lieberman 漿細(xì)胞瘤、B16 黑色素瘤、結(jié)腸腫瘤 26 和 Ridgway 成骨肉瘤[3]。
Bisantrene 在 1.56 至 150 mg/kg 的劑量范圍內(nèi)有效,具體取決于處理的頻率、途徑和時(shí)間表以及使用的腫瘤模型[3]。
Bisantrene (25,50 和 100 mg/kg;腹腔注射;once) 預(yù)處理巨噬細(xì)胞對(duì)注射 P815 腫瘤細(xì)胞的小鼠顯示出抗腫瘤作用[3]。
Bisantrene (10-150 mg/kg;靜脈注射;一次) 在 Neo 小鼠中劑量依賴性地誘導(dǎo)白細(xì)胞減少。B 細(xì)胞和巨噬細(xì)胞是 Bisantrene 毒性的靶標(biāo)[4]

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

Clinical Trial
分子量

398.46

Formula

C22H22N8

CAS 號(hào)
性狀

固體

顏色

Orange to red

中文名稱

比生群;必桑郡

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 1 mg/mL (2.51 mM; 超聲助溶 (<80°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5097 mL 12.5483 mL 25.0966 mL
5 mM --- --- ---
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 98.08%

參考文獻(xiàn)
Kinase Assay
[1]

Measurements are carried out at 25°C in ETN buffer (1 mM EDTA, 10 mM Tris, pH 7.0, with NaCl to obtain the desired ionic strength). Binding is monitored spectrophotometrically or fluorometrically, in the ligand absorption or emission region, respectively, after addition of scalar amounts of DNA to a freshly prepared drug solution. To avoid large systematic inaccuracies resulting from experimental errors in extinction coefficients or fluorescence quantum yield, the range of bound drug fractions is 0.15-0.85. Data are evaluated. Spectroscopic measurements are made with a Perkin-Elmer Lambda 5 apparatus and a MPF66 fluorometer, both equipped with a Haake F3-C thermostat[1].

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

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5097 mL 12.5483 mL 25.0966 mL 62.7416 mL
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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產(chǎn)品名稱:
Bisantrene
目錄號(hào):
HY-100875
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