Microtubule inhibitor 2

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Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity.

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Microtubule inhibitor 2 Chemical Structure

CAS No. : 3031328-45-4

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.02 μM Compound: 33	Antiproliferative activity against human A2780 cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 35282680]
A2780	IC₅₀	0.04 μM Compound: 33	Antiproliferative activity against human paclitaxel-resistant A2780/TAX cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human paclitaxel-resistant A2780/TAX cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 35282680]
A549	IC₅₀	0.01 μM Compound: 33	Antiproliferative activity against human A549 cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 35282680]
A549	IC₅₀	0.01 μM Compound: 33	Cytotoxicity against human A549 cells assessed as reduction in cell viability Cytotoxicity against human A549 cells assessed as reduction in cell viability	[PMID: 35282680]
A549	IC₅₀	0.02 μM Compound: 33	Antiproliferative activity against human adriamycin-resistant A549/ADR cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human adriamycin-resistant A549/ADR cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 35282680]
HCT-8	IC₅₀	0.04 μM Compound: 33	Antiproliferative activity against human HCT-8 cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-8 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 35282680]
HCT-8	IC₅₀	0.07 μM Compound: 33	Antiproliferative activity against human vincristine-resistant HCT-8/VCR cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human vincristine-resistant HCT-8/VCR cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 35282680]
HUVEC	IC₅₀	0.04 μM Compound: 33	Cytotoxicity against HUVEC cells assessed as reduction in cell viability Cytotoxicity against HUVEC cells assessed as reduction in cell viability	[PMID: 35282680]
HeLa	IC₅₀	0.02 μM Compound: 33	Antiproliferative activity against human HeLa cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 35282680]
L02	IC₅₀	1.45 μM Compound: 33	Cytotoxicity against human L02 cells assessed as reduction in cell viability Cytotoxicity against human L02 cells assessed as reduction in cell viability	[PMID: 35282680]
MCF-10A	IC₅₀	0.54 μM Compound: 33	Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability	[PMID: 35282680]
MCF7	IC₅₀	0.05 μM Compound: 33	Antiproliferative activity against human MCF7 cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 35282680]

In Vitro

Microtubule inhibitor 2 (compound 33) (48 h) shows antiproliferative activity with IC₅₀ values of 0.01, 0.02, 0.02, 0.04, 0.05 µM for A549, Hela, A2780, HCT-8, MCF-7 cells, respectively^[1].
Microtubule inhibitor 2 shows selective toward normal human cells and cancer cells (IC₅₀s of 0.01, 0.04, 1.45, 1.32,0.54 µM for A549, quiescent HUVECs, LO2, HLF, MCF-10A cells, respectively)^[1].
Microtubule inhibitor 2 (48 h) shows antiproliferative activity toward drug-resistant cancer cells (IC₅₀s of 0.02, 0.07, 0.04 for A549/ADM, HCT-8/VCR, A2780/TAX cells, respectively)^[1].
Microtubule inhibitor 2 (5, 10, 20 nM; 24 h) dramatically disrupts the dynamic balance of the tubulin−microtubule system, induces the multipolarization of the mitotic spindle, and interfered with the mitosis of A549 cells^[1].
Microtubule inhibitor 2 (5, 10, 20 nM, 24 h, 48 h) arrests cell cycle progression at the G2/M phase in a dose and time-dependent manner^[1].
Microtubule inhibitor 2 triggers cell death through ferroptosis rather than apoptosis^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	A549, Hela, A2780, HCT-8, MCF-7 cells
Concentration:
Incubation Time:	48 h
Result:	Showed antiproliferative activities with IC₅₀ values of 0.01, 0.02, 0.02, 0.04, 0.05 µM for A549, Hela, A2780, HCT-8, MCF-7 cells, respectively.

Cell Cycle Analysis^[1]

Cell Line:	A549 cells
Concentration:	5, 10, 20 nM
Incubation Time:	24 h, 48 h
Result:	Arrested cell cycle progression at the G2/M phase in a dose and time-dependent manner.

In Vivo

Microtubule inhibitor 2 (10 mg/kg; p.o.)displays excellent oral bioavailability (F% = 69.45) ^[1].
Microtubule inhibitor 2 (10 mg/kg; i.p.; every other day for 22 days) shows antitumor activity and the level of tumor growth inhibition was 78.63%^[1].
Pharmacokinetic Parameters of Microtubule inhibitor 2 in Male Institute of Cancer Research (ICR) mice (18−23 g)^[1].

	p.o.	i.v.
dose (mg/kg)	10	1
T_1/2 (h)	2.12	0.62
T_max (h)	0.25	0.08
T_max (ng/mL)	776.31	871.40
AUC_(0-t) (h ng^-1 mL)	2432.04	350.19
AUC_(0-∞) (h ng^-1 mL)	2463.76	353.02
MRT (h)	2.57	0.68
CL (mL h^-1 kg^-1)	-	2855.67
F %	69.45	-

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

Animal Model:	Male Institute of Cancer Research (ICR) mice (18−23 g) ^[1]
Dosage:	10 mg/kg
Administration:
Result:	Displayed excellent oral bioavailability (F% = 69.45).

Animal Model:	Male BALB/c nude mice (5 weeks old, 18−20 g) (A549 xenograft models) ^[1]
Dosage:	10 mg/kg
Administration:	i.p.; every other day, 22 days
Result:	Showed antitumor activity and the level of tumor growth inhibition was 78.63%.

Molecular Weight

389.40

Formula

C₂₀H₂₃NO₇

CAS No.

3031328-45-4

SMILES

C=C(C1=CC=C(C(O)=C1NC(CO)=O)OC)C2=CC(OC)=C(C(OC)=C2)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Zhou J, et al. Discovery of a Novel Stilbene Derivative as a Microtubule Targeting Agent Capable of Inducing Cell Ferroptosis. J Med Chem. 2022; 65(6):4687-4708. [Content Brief]