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

Indimitecan (LMP776) 是一種拓?fù)洚悩?gòu)酶 I (Top1) 抑制劑,具有抗癌活性。

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Indimitecan Chemical Structure

Indimitecan Chemical Structure

CAS No. : 915360-05-3

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Other Forms of Indimitecan:

查看 Topoisomerase 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities[1].

IC50 & Target

Top1

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
DU-145 GI50
< 0.01 μM
Compound: 7, indimitecan
Antiproliferative activity against human DU145 cells by SRB assay
Antiproliferative activity against human DU145 cells by SRB assay
[PMID: 21710981]
HCT-116 GI50
< 0.01 μM
Compound: 7, indimitecan
Antiproliferative activity against human HCT116 cells by SRB assay
Antiproliferative activity against human HCT116 cells by SRB assay
[PMID: 21710981]
HOP-62 GI50
< 0.01 μM
Compound: 7, indimitecan
Antiproliferative activity against human HOP62 cells by SRB assay
Antiproliferative activity against human HOP62 cells by SRB assay
[PMID: 21710981]
L1210 EC50
0.06 μM
Compound: 19
Trypanocidal activity against Trypanosoma brucei brucei 427 bloodstream forms infected in mouse L1210 cells after 48 hrs
Trypanocidal activity against Trypanosoma brucei brucei 427 bloodstream forms infected in mouse L1210 cells after 48 hrs
[PMID: 18824603]
MCF7 GI50
0.01 μM
Compound: 7, indimitecan
Antiproliferative activity against human MCF7 cells by SRB assay
Antiproliferative activity against human MCF7 cells by SRB assay
[PMID: 21710981]
OVCAR-3 GI50
0.085 μM
Compound: 7, indimitecan
Antiproliferative activity against human OVCAR3 cells by SRB assay
Antiproliferative activity against human OVCAR3 cells by SRB assay
[PMID: 21710981]
SF-539 GI50
0.037 μM
Compound: 7, indimitecan
Antiproliferative activity against human SF539 cells by SRB assay
Antiproliferative activity against human SF539 cells by SRB assay
[PMID: 21710981]
SN12C GI50
< 0.01 μM
Compound: 7, indimitecan
Antiproliferative activity against human SN12C cells by SRB assay
Antiproliferative activity against human SN12C cells by SRB assay
[PMID: 21710981]
UACC-62 GI50
< 0.01 μM
Compound: 7, indimitecan
Antiproliferative activity against human UACC62 cells by SRB assay
Antiproliferative activity against human UACC62 cells by SRB assay
[PMID: 21710981]
體外研究
(In Vitro)

Indimitecan (LMP776) (0-100 μM) 顯示出對(duì)多種人類(lèi)癌細(xì)胞系的抗增殖效力,平均圖中點(diǎn) (MGM) 為 0.079 ± 0.023 μM[1]。
Indimitecan 顯示由于 Top1 抑制[1],可有效切割 DNA。
Indimitecan 可以作為代謝酮還原酶的底物[1]。

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

Cell Proliferation Assay[1]

Cell Line: HOP-62, HCT-116, SF-539, UACC-62, OVCAR-3, SN12C, DU-145, MCF-7
Concentration: 0-100 μM
Incubation Time:
Result: Showed growth inhibition with GI50s of <0.01, <0.01, 0.04, <0.01, 0.08, <0.01, <0.01 and 0.01 μM against HOP-62, HCT-116, SF-539, UACC-62, OVCAR-3, SN12C, DU-145 and MCF-7 cells, respectively. And the mean-graph midpoint (MGM) for growth inhibition of all human cancer cell lines successfully tested (the National Cancer Institute’s developmental therapeutics assay (the “NCI60”)) was 0.079 ± 0.023 μM.
Clinical Trial
分子量

459.45

Formula

C25H21N3O6

CAS 號(hào)
性狀

固體

顏色

Brown to black

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 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 8.33 mg/mL (18.13 mM; 超聲助溶 (<60 ℃);酸性條件溶解 (HCL 調(diào)節(jié),pH=3) ; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.1765 mL 10.8826 mL 21.7652 mL
5 mM 0.4353 mL 2.1765 mL 4.3530 mL
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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(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(guò)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: 98.03%

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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(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 2.1765 mL 10.8826 mL 21.7652 mL 54.4129 mL
5 mM 0.4353 mL 2.1765 mL 4.3530 mL 10.8826 mL
10 mM 0.2177 mL 1.0883 mL 2.1765 mL 5.4413 mL
15 mM 0.1451 mL 0.7255 mL 1.4510 mL 3.6275 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(chēng):
Indimitecan
目錄號(hào):
HY-18350
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