1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  2. Microtubule/Tubulin Apoptosis
  3. Tubulin polymerization-IN-9

Tubulin polymerization-IN-9 is a potent tubulin inhibitor with IC50 of 1.82 μM. Tubulin polymerization-IN-9 causes cell cycle arrest at G2/M phase, and induces cell apoptosis and depolarized mitochondria of K562 cells. Tubulin polymerization-IN-9 has potent anti-vascular and antitumor activities.

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Tubulin polymerization-IN-9 Chemical Structure

Tubulin polymerization-IN-9 Chemical Structure

CAS No. : 2485020-93-5

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Description

Tubulin polymerization-IN-9 is a potent tubulin inhibitor with IC50 of 1.82 μM. Tubulin polymerization-IN-9 causes cell cycle arrest at G2/M phase, and induces cell apoptosis and depolarized mitochondria of K562 cells. Tubulin polymerization-IN-9 has potent anti-vascular and antitumor activities[1].

IC50 & Target

IC50: 1.82 μM (tubulin)[1]

In Vitro

Tubulin polymerization-IN-9 (compound 11k) (0.1, 1, 10 μM; 72 hours) has potent activity against these three cancer cell lines with IC50 values ranging from 0.287 to 0.621 μM[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 24 hours) induces a dose-dependent collapse of the microtubule networks[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 48 hours) observes a gradual accumulation of cells at G2/M phase in K562 cells[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 72 hours) effectively induces cell apoptosis in K562 cells in a concentration-dependent manner[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 24 hours) causes mitochondrial depolarization of K562 cells in the process of apoptosis[1].

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

Cell Proliferation Assay

Cell Line: K562 HepG2 and HCT-8 cells[1]
Concentration: 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Showed potent activity against these three cancer cell lines with IC50 values ranging from 0.287 to 0.621 μM.

Immunofluorescence

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 24 hours
Result: Induced a dose-dependent collapse of the microtubule networks.

Cell Cycle Analysis

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 48 hours
Result: Observed a gradual accumulation of cells at G2/M phase in K562 cells.

Apoptosis Analysis

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 72 hours
Result: Effectively induced cell apoptosis in K562 cells in a concentration-dependent manner.
In Vivo

Tubulin polymerization-IN-9 (15 and 30 mg/kg; IV; once a day, for 21 days) effectively suppresses the tumor volume and reduces tumor weight by 71.1% at a dose of 30 mg/kg[1].

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

Animal Model: Male ICR mice (5 weeks; injected with H22 cells; n=6)[1]
Dosage: 15 and 30 mg/kg
Administration: IV; once a day, for 21 days
Result: Effectively suppressed the tumor volume and reduced tumor weight by 71.1% at a dose of 30 mg/kg.
Molecular Weight

420.32

Formula

C19H19NO5Se

CAS No.
SMILES

COC1=CC([Se](=O)(/C=C/C2=CC=CC3=C2C=CN3)=O)=CC(OC)=C1OC

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Purity & Documentation
References
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Tubulin polymerization-IN-9
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