Verubulin
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.85%
- CAS No.: 827031-83-4
- Formula: C17H17N3O
- Molecular Weight:279.34
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Microtubule[1]
|
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 | 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 |
0.004 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 | 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: 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 |
0.005 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 |
0.006 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: 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-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-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] |
| NCI-H1299 | EC50 |
0.007 μM
Compound: 1g
|
Induction of apoptosis in human H1299 cells assessed as caspase activation
Induction of apoptosis in human H1299 cells assessed as caspase activation
|
[PMID: 20188546] |
| 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: 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 | 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: 1g
|
Induction of apoptosis in human T47D cells assessed as caspase activation
Induction of apoptosis in human T47D cells assessed as caspase activation
|
[PMID: 20188546] |
| 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] |
Verubulin (10 nM; 1-3 h) rapidly disrupts microtubule formation in human A549 non-small-cell lung carcinoma cells[2].
Verubulin inhibits the growth of MCF-7 cells with an IC50 value of 2.1 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic mice (nu/nu), B16 mouse melanoma or OVCAR3 human ovarian cancer cell-implanted subcutaneous xenograft models[3]
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Dosage:1 mg/kg, 7.5 mg/kg (B16); 2.5, 5 or 10 mg/kg (OVCAR-3)
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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).
Chemical Information
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CAS No. 827031-83-4
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Appearance Solid
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Molecular Weight 279.34
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Formula C17H17N3O
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Color Light yellow to yellow
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SMILES
CC1=NC(N(C2=CC=C(OC)C=C2)C)=C3C=CC=CC3=N1
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Synonyms
MPC 6827
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (357.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Kasibhatla S, et al. MPC-6827: a small-molecule inhibitor of microtubule formation that is not a substrate for multidrug resistance pumps. Cancer Res. 2007 Jun 15;67(12):5865-71. [Content Brief]
[2]. Kasibhatla S, et al. MPC-6827: a small-molecule inhibitor of microtubule formation that is not a substrate for multidrug resistance pumps. Cancer Res. 2007 Jun 15;67(12):5865-71. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 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 |