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

Verubulin  (Synonyms: MPC 6827)

目录号: HY-14907 纯度: 99.34%
COA 产品使用指南 技术支持

Verubulin (MPC-6827) 是一种高效、广谱的微管 (microtubule) 阻断剂。Verubulin 对乳腺癌、黑色素瘤和卵巢癌具有抗肿瘤活性。Verubulin 可用于非小细胞肺癌研究。

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Verubulin

Verubulin Chemical Structure

CAS No. : 827031-83-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥880
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5 mg ¥800
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10 mg ¥1350
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50 mg ¥4750
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Other Forms of Verubulin:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Verubulin (MPC-6827) is a highly potent and broad-spectrum microtubule blocker. Verubulin has antitumor activity against breast cancer, melanoma, and ovarian cancer. Verubulin can be used in non-small cell lung cancer research[1][2][3].

IC50 & Target

Microtubule[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-375 IC50
0.7 nM
Compound: Verubulin
Antiproliferative activity against human A-375 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
Antiproliferative activity against human A-375 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
[PMID: 34406768]
A375/TxR IC50
0.7 nM
Compound: Verubulin
Antiproliferative activity against human A375/TxR cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
Antiproliferative activity against human A375/TxR cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
[PMID: 34406768]
A-431 IC50
0.9 nM
Compound: 1
Cytotoxicity against human A-431 cells assessed as reduction in cell viability by Sulforhodamine B assay
Cytotoxicity against human A-431 cells assessed as reduction in cell viability by Sulforhodamine B assay
[PMID: 33647840]
A549 IC50
0.003 μM
Compound: EP128495
Growth inhibition of human A549 cells after 48 hrs by MTT assay
Growth inhibition of human A549 cells after 48 hrs by MTT assay
[PMID: 29509413]
A549 IC50
0.004 μM
Compound: MPC-6827
Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay
[PMID: 29673981]
A549 IC50
0.005 μM
Compound: MPC6827
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
[PMID: 30093295]
A549/CDDP IC50
0.009 μM
Compound: EP128495
Growth inhibition of human A549/CDDP cells after 48 hrs by MTT assay
Growth inhibition of human A549/CDDP cells after 48 hrs by MTT assay
[PMID: 29509413]
BJ IC50
0.015 μM
Compound: EP128495
Antiproliferative activity against human BJ cells after 48 hrs by MTT assay
Antiproliferative activity against human BJ cells after 48 hrs by MTT assay
[PMID: 29509413]
HCT-116 EC50
0.003 μM
Compound: 6h, EP128495,MPC-6827, azixa
Induction of apoptosis in human HCT116 cells assessed as caspase activation after 24 hrs by HTS assay
Induction of apoptosis in human HCT116 cells assessed as caspase activation after 24 hrs by HTS assay
[PMID: 19296653]
HCT-116 IC50
0.004 μM
Compound: EP128495
Growth inhibition of human HCT116 cells after 48 hrs by MTT assay
Growth inhibition of human HCT116 cells after 48 hrs by MTT assay
[PMID: 29509413]
HCT-116 IC50
0.005 μM
Compound: MPC-6827
Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay
[PMID: 29673981]
HCT-116 GI50
0.006 μM
Compound: 6h, EP128495,MPC-6827, azixa
Growth inhibition of human HCT116 cells after 48 hrs by celltiter assay
Growth inhibition of human HCT116 cells after 48 hrs by celltiter assay
[PMID: 19296653]
HCT-116 IC50
0.009 μM
Compound: MPC6827
Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
[PMID: 30093295]
HCT-116 IC50
4.3 nM
Compound: 5; MPC-6827
Antiproliferative activity against human HCT116 cells after 24 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 24 hrs by MTT assay
[PMID: 27213819]
HeLa IC50
0.005 μM
Compound: EP128495
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
[PMID: 29509413]
HeLa IC50
0.006 μM
Compound: MPC-6827
Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay
[PMID: 29673981]
HeLa IC50
0.007 μM
Compound: MPC6827
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
[PMID: 30093295]
HeLa IC50
1.5 nM
Compound: 1
Cytotoxicity against human HeLa cells over expressing WT-beta3 assessed as reduction in cell viability by Sulforhodamine B assay
Cytotoxicity against human HeLa cells over expressing WT-beta3 assessed as reduction in cell viability by Sulforhodamine B assay
[PMID: 33647840]
HeLa IC50
2 nM
Compound: 1
Cytotoxicity against human HeLa cells assessed as reduction in cell viability by Sulforhodamine B assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability by Sulforhodamine B assay
[PMID: 33647840]
HepG2 IC50
0.005 μM
Compound: MPC-6827
Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay
[PMID: 29673981]
HepG2 IC50
0.005 μM
Compound: EP128495
Growth inhibition of human HepG2 cells after 48 hrs by MTT assay
Growth inhibition of human HepG2 cells after 48 hrs by MTT assay
[PMID: 29509413]
HepG2 IC50
0.006 μM
Compound: MPC6827
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 30093295]
HepG2 IC50
4.6 nM
Compound: 5; MPC-6827
Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay
[PMID: 27213819]
L02 IC50
0.013 μM
Compound: EP128495
Antiproliferative activity against human LO2 cells after 48 hrs by MTT assay
Antiproliferative activity against human LO2 cells after 48 hrs by MTT assay
[PMID: 29509413]
LoVo IC50
0.008 μM
Compound: EP128495
Growth inhibition of human LoVo cells after 48 hrs by MTT assay
Growth inhibition of human LoVo cells after 48 hrs by MTT assay
[PMID: 29509413]
M14 IC50
1 nM
Compound: Verubulin
Antiproliferative activity against human M14 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
Antiproliferative activity against human M14 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
[PMID: 34406768]
MCF7 IC50
0.011 μM
Compound: EP128495
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
[PMID: 29509413]
MDA-MB-231 IC50
0.008 μM
Compound: MPC-6827
Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay
[PMID: 29673981]
MDA-MB-231 IC50
0.008 μM
Compound: EP128495
Growth inhibition of human MDA-MB-231 cells after 48 hrs by MTT assay
Growth inhibition of human MDA-MB-231 cells after 48 hrs by MTT assay
[PMID: 29509413]
MDA-MB-435 IC50
1.7 nM
Compound: 1
Antiproliferative activity against human MDA-MB-435 cells assessed as reduction in cell viability by Sulforhodamine B assay
Antiproliferative activity against human MDA-MB-435 cells assessed as reduction in cell viability by Sulforhodamine B assay
[PMID: 33647840]
MGC-803 IC50
0.008 μM
Compound: EP128495
Antiproliferative activity against human MGC803 cells after 48 hrs by MTT assay
Antiproliferative activity against human MGC803 cells after 48 hrs by MTT assay
[PMID: 29509413]
NCI-H1299 EC50
0.006 μM
Compound: 1e
Induction of apoptosis in human H1299 cells assessed as caspase activation after 48 hrs by HTS assay
Induction of apoptosis in human H1299 cells assessed as caspase activation after 48 hrs by HTS assay
[PMID: 19464890]
RKO IC50
0.003 μM
Compound: EP128495
Growth inhibition of human RKO cells after 48 hrs by MTT assay
Growth inhibition of human RKO cells after 48 hrs by MTT assay
[PMID: 29509413]
RKO IC50
0.005 μM
Compound: MPC6827
Antiproliferative activity against human RKO cells after 48 hrs by MTT assay
Antiproliferative activity against human RKO cells after 48 hrs by MTT assay
[PMID: 30093295]
SK-OV-3 IC50
2.2 nM
Compound: 1
Cytotoxicity against human SK-OV-3 cells assessed as reduction in cell viability by Sulforhodamine B assay
Cytotoxicity against human SK-OV-3 cells assessed as reduction in cell viability by Sulforhodamine B assay
[PMID: 33647840]
SK-OV-3 IC50
2.6 nM
Compound: 1
Cytotoxicity against human SK-OV-3 cells over expressing MDR1-6/6 assessed as reduction in cell viability by Sulforhodamine B assay
Cytotoxicity against human SK-OV-3 cells over expressing MDR1-6/6 assessed as reduction in cell viability by Sulforhodamine B assay
[PMID: 33647840]
SK-OV-3 IC50
3.2 nM
Compound: 5; MPC-6827
Antiproliferative activity against human SKOV3 cells after 24 hrs by MTT assay
Antiproliferative activity against human SKOV3 cells after 24 hrs by MTT assay
[PMID: 27213819]
SNU-398 EC50
0.002 μM
Compound: 6h, EP128495,MPC-6827, azixa
Induction of apoptosis in human SNU398 cells assessed as caspase activation after 24 hrs by HTS assay
Induction of apoptosis in human SNU398 cells assessed as caspase activation after 24 hrs by HTS assay
[PMID: 19296653]
SNU-398 GI50
0.003 μM
Compound: 6h, EP128495,MPC-6827, azixa
Growth inhibition of human SNU398 cells after 48 hrs by celltiter assay
Growth inhibition of human SNU398 cells after 48 hrs by celltiter assay
[PMID: 19296653]
T47D EC50
0.002 μM
Compound: 6h, EP128495,MPC-6827, azixa
Induction of apoptosis in human T47D cells assessed as caspase activation after 24 hrs by HTS assay
Induction of apoptosis in human T47D cells assessed as caspase activation after 24 hrs by HTS assay
[PMID: 19296653]
T47D EC50
0.002 μM
Compound: 1e
Induction of apoptosis in human T47D cells assessed as caspase activation after 48 hrs by HTS assay
Induction of apoptosis in human T47D cells assessed as caspase activation after 48 hrs by HTS assay
[PMID: 19464890]
T47D GI50
0.006 μM
Compound: 6h, EP128495,MPC-6827, azixa
Growth inhibition of human T47D cells after 48 hrs by celltiter assay
Growth inhibition of human T47D cells after 48 hrs by celltiter assay
[PMID: 19296653]
U-251 IC50
2.8 nM
Compound: 1
Cytotoxicity against human U-251 cells assessed as reduction in cell viability by Sulforhodamine B assay
Cytotoxicity against human U-251 cells assessed as reduction in cell viability by Sulforhodamine B assay
[PMID: 33647840]
体外研究
(In Vitro)

Verubulin (10 nM;1-3 h) 可快速破坏人 A549 非小细胞肺癌细胞中的微管形成[2]
Verubulin (72 h) 可抑制 MCF-7 细胞的生长,IC50 值为 2.1 nM[2]

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

体内研究
(In Vivo)

Verubulin (7.5 mg/kg;静脉注射;一次或 1 mg/kg;静脉注射;5 天) 可在 B16 小鼠黑色素瘤模型中诱导肿瘤生长抑制[3]

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

Animal Model: Athymic mice (nu/nu), B16 mouse melanoma or OVCAR3 human ovarian cancer cell-implanted subcutaneous xenograft models[3]
Dosage: 1 mg/kg, 7.5 mg/kg (B16); 2.5, 5 or 10 mg/kg (OVCAR-3)
Administration: In the B16 study, 7.5 mg/kg was dosed intravenously (i.v.) once, or 1 mg/kg was dosed daily for five days. In the OVCAR-3 study, 5 mg/kg was dosed i.v. once, or 2.5-10 mg/kg/day was dosed intraperitoneally (i.p.) with an Alzet mini-pump for one day.
Result: Resulted in 72% tumor growth inhibition (TGI) on day 7 relative to vehicle at 7.5 mg/kg dose (in the B16 model).
Resulted in only 22% TGI (at the 1 mg/kg daily dosing for five days) (in the B16 model).
Did not result in inhibition of xenograft tumor growth relative to vehicle at day 17 when administered intraperitoneally at a dose of 2.5 mg/kg for 24 hours (in the OVCAR-3 model).
Resulted in 50% regression at single 5 mg/kg dose (i.v.) (in the OVCAR-3 model).
Showed median time to tumor volume of 1500 mm3: 28.5 days (2.5 mg/kg/day i.p. group); > 39 days (5 mg/kg i.v. group).
Clinical Trial
分子量

279.34

Formula

C17H17N3O

CAS 号
性状

固体

颜色

Light yellow to 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 : 100 mg/mL (357.99 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 3.5799 mL 17.8993 mL 35.7987 mL
5 mM 0.7160 mL 3.5799 mL 7.1597 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

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (7.45 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (7.45 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
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
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.34%

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 3.5799 mL 17.8993 mL 35.7987 mL 89.4967 mL
5 mM 0.7160 mL 3.5799 mL 7.1597 mL 17.8993 mL
10 mM 0.3580 mL 1.7899 mL 3.5799 mL 8.9497 mL
15 mM 0.2387 mL 1.1933 mL 2.3866 mL 5.9664 mL
20 mM 0.1790 mL 0.8950 mL 1.7899 mL 4.4748 mL
25 mM 0.1432 mL 0.7160 mL 1.4319 mL 3.5799 mL
30 mM 0.1193 mL 0.5966 mL 1.1933 mL 2.9832 mL
40 mM 0.0895 mL 0.4475 mL 0.8950 mL 2.2374 mL
50 mM 0.0716 mL 0.3580 mL 0.7160 mL 1.7899 mL
60 mM 0.0597 mL 0.2983 mL 0.5966 mL 1.4916 mL
80 mM 0.0447 mL 0.2237 mL 0.4475 mL 1.1187 mL
100 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8950 mL
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  • 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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目录号:
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