Art. -Nr.: HY-14907

Verubulin

Name: Verubulin
Brand: MedChemExpress
SKU: HY-14907
Price: 80.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: MPC 6827)

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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.

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Reinheit: 99.85%
CAS. Nr.: 827031-83-4
Formel: C₁₇H₁₇N₃O
Molecular Weight:279.34

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Verubulin Chemical Structure

CAS. Nr.: 827031-83-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Microtubule^[1]

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	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]

In Vitro

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.

In Vivo

Verubulin (7.5 mg/kg; i.v.; once or 1 mg/kg; i.v.; 5 days) induces tumor growth inhibition in B16 mouse melanoma model^[3].

MedChemExpress (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).

Chemical Information

CAS. Nr. 827031-83-4
Appearance Solid
Molecular Weight 279.34
Formel C₁₇H₁₇N₃O
Color Light yellow to yellow
SMILES

CC1=NC(N(C2=CC=C(OC)C=C2)C)=C3C=CC=CC3=N1
Synonyms

MPC 6827
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.5799 mL

17.8993 mL

35.7987 mL

5 mM

0.7160 mL

3.5799 mL

7.1597 mL

10 mM

0.3580 mL

1.7899 mL

3.5799 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (7.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

[3]. Jones J T, et al. Comparison of MPC-6827 activity in xenograft models with different dosing schedules. Journal of Clinical Oncology, 2011, 29(15_suppl): e13080-e13080.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Verubulin

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Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

Verubulin

Doxorubicin hydrochloride

Volasertib

BNC105

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

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