1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  2. Microtubule/Tubulin Apoptosis
  3. MPT0B014

MPT0B014  (Synonyms: 6-(3′,4′,5′-Trimethoxybenzoyl)quinoline)

目录号: HY-120786 纯度: 99.67%
COA 产品使用指南

MPT0B014 是一种微管蛋白聚合 (tubulin polymerization) 抑制剂。MPT0B014 诱导癌细胞凋亡 (apoptosis)。MPT0B014 可用于癌症研究。

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MPT0B014 Chemical Structure

MPT0B014 Chemical Structure

CAS No. : 1215208-59-5

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10 mM * 1 mL in DMSO ¥407
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5 mg ¥370
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10 mg ¥600
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MPT0B014 is a tubulin polymerization inhibitor. MPT0B014 induces cancer cell apoptosis. MPT0B014 can be used for the research of cancer[1].

IC50 & Target

Tubulin polymerization[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HT-29 IC50
24.6 nM
Compound: 9
Antiproliferative activity against human HT-29 cells after 72 hrs by methylene blue dye assay
Antiproliferative activity against human HT-29 cells after 72 hrs by methylene blue dye assay
[PMID: 20148562]
KB IC50
24 nM
Compound: 9
Antiproliferative activity against human KB cells after 72 hrs by methylene blue dye assay
Antiproliferative activity against human KB cells after 72 hrs by methylene blue dye assay
[PMID: 20148562]
MKN-45 IC50
16.3 nM
Compound: 9
Antiproliferative activity against human MKN45 cells after 72 hrs by methylene blue dye assay
Antiproliferative activity against human MKN45 cells after 72 hrs by methylene blue dye assay
[PMID: 20148562]
NCI-H460 IC50
36 nM
Compound: 9
Antiproliferative activity against human H460 cells after 72 hrs by methylene blue dye assay
Antiproliferative activity against human H460 cells after 72 hrs by methylene blue dye assay
[PMID: 20148562]
体外研究
(In Vitro)

MPT0B014 (0-1 μM; 48 h) 以剂量依赖的方式抑制 A549、H1299 和 H226 细胞的生长[1]
MPT0B014 (0.05-0.3 μM; 24 and 48 h) 在 A549 细胞中使细胞周期阻滞于 G2/M 期和 sub-G1 期,诱导细胞凋亡[1]

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

Cell Viability Assay[1]

Cell Line: A549, H1299, H226 and HUVEC cells
Concentration: 0, 0.025, 0.05, 0.075 and 1 μM
Incubation Time: 48 h
Result: Inhibited cell viability with IC50s of 0.109±0.01, 0.055±0.004, 0.077±0.005 and 0.536±0.166 μM against A549, H1299, H226 and HUVEC cells, respectively.

Cell Cycle Analysis[1]

Cell Line: A549, H1299 and H226
Concentration: 0.05, 0.1 and 0.3 μM
Incubation Time: 24 and 48 h
Result: Treatment for 24 h led to notable accumulation of cells in the G2/M phase. At 48 h, sub-G1 apoptotic cell populations were increased in a concentration-dependent manner. Cells in the G2/M phase began to rise at 12 h post-treatment and peaked at 24 h. Following this, there was an emergence of cells in the sub-G1 population phase until 48 h.

Western Blot Analysis[1]

Cell Line: A549, H1299 and H226
Concentration: 0.05, 0.1 and 0.3 μM
Incubation Time: 24 h
Result: Resulted in a marked increase in expression of the mitosis marker MPM2 and the proteins cyclin B1, Cdc2, Thr161, Aurora A and Aurora B in a concentration-dependent manner. Decreased the expression of Cdc (Tyr15) and Cdc25C, whereas total protein levels of Cdc2 did not change.

Apoptosis Analysis[1]

Cell Line: A549
Concentration: 0.05, 0.075, 0.1 and 0.3 μM
Incubation Time: 48 h
Result: Induced apoptosis in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: A549
Concentration: 0.05, 0.1 and 0.3 μM
Incubation Time: 24, 36 and 48 h
Result: Induced activation of caspases-3, -7, -8 and -9, and cleavage of PARP in a time- and concentration-dependent manner. Significantly induced Bcl-2 phosphorylation. Down-regulated Mcl-1 expression in a concentration-dependent manner.
体内研究
(In Vivo)

MPT0B014 (100 mg/kg; i.v./i.p.; daily for 25 days) 和 25 mg/kg Erlotinib (HY-50896) 联用显著改善小鼠 A549 肿瘤抑制[1]

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

Animal Model: Nude athymic mice, A549 xenografts[1]
Dosage: 100 mg/kg alone or in combination with 25 mg/kg Erlotinib (HY-50896)
Administration: i.v./i.p., daily for 25 days
Result: The combined treatment resulted in more significant tumor growth delay (28%) compared with treatment alone (7%). The combination produced significantly higher anti-tumor activity. The growth of A549 cancer cell xenografts was suppressed by 11, 21 and 49% (tumor growth inhibition) after treatment with MPT0B014, Erlotinib and MPT0B014 plus Erlotinib, respectively.
分子量

323.34

Formula

C19H17NO4

CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (154.64 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0927 mL 15.4636 mL 30.9272 mL
5 mM 0.6185 mL 3.0927 mL 6.1854 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0927 mL 15.4636 mL 30.9272 mL 77.3180 mL
5 mM 0.6185 mL 3.0927 mL 6.1854 mL 15.4636 mL
10 mM 0.3093 mL 1.5464 mL 3.0927 mL 7.7318 mL
15 mM 0.2062 mL 1.0309 mL 2.0618 mL 5.1545 mL
20 mM 0.1546 mL 0.7732 mL 1.5464 mL 3.8659 mL
25 mM 0.1237 mL 0.6185 mL 1.2371 mL 3.0927 mL
30 mM 0.1031 mL 0.5155 mL 1.0309 mL 2.5773 mL
40 mM 0.0773 mL 0.3866 mL 0.7732 mL 1.9329 mL
50 mM 0.0619 mL 0.3093 mL 0.6185 mL 1.5464 mL
60 mM 0.0515 mL 0.2577 mL 0.5155 mL 1.2886 mL
80 mM 0.0387 mL 0.1933 mL 0.3866 mL 0.9665 mL
100 mM 0.0309 mL 0.1546 mL 0.3093 mL 0.7732 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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产品名称:
MPT0B014
目录号:
HY-120786
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