2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. Tubulin polymerization-IN-92

Tubulin polymerization-IN-92, an analog of KX-01 (HY-10340), is a potent orally active tubulin polymerization inhibitor that binds tubulin with a Ka of 1.29 μM. Tubulin polymerization-IN-92 simultaneously occupies the colchicine site in β-tubulin and a cavity in α-tubulin. Tubulin polymerization-IN-92 exerts antiproliferative activity, induces G2/M cell cycle arrest and apoptosis in cancer cells. Tubulin polymerization-IN-92 inhibits tumor growth in mouse xenograft models. Tubulin polymerization-IN-92 can be used for the research of colon cancer, cervical cancer, and Paclitaxel (HY-B0015)-resistant ovarian cancer.

For research use only. We do not sell to patients.

Tubulin polymerization-IN-92

Tubulin polymerization-IN-92 Chemical Structure

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Tubulin polymerization-IN-92 Related Antibodies

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Description

Tubulin polymerization-IN-92, an analog of KX-01 (HY-10340), is a potent orally active tubulin polymerization inhibitor that binds tubulin with a Ka of 1.29 μM. Tubulin polymerization-IN-92 simultaneously occupies the colchicine site in β-tubulin and a cavity in α-tubulin. Tubulin polymerization-IN-92 exerts antiproliferative activity, induces G2/M cell cycle arrest and apoptosis in cancer cells. Tubulin polymerization-IN-92 inhibits tumor growth in mouse xenograft models. Tubulin polymerization-IN-92 can be used for the research of colon cancer, cervical cancer, and Paclitaxel (HY-B0015)-resistant ovarian cancer[1].

In Vitro

Tubulin polymerization-IN-92 (compound 8h) potently inhibits proliferation of HCT116, HeLa, A2780S, A2780T, HT29, and HUVEC cells with IC50 values of 3.5, 2.4, 15.7, 22.1, and 7.3 nM, respectively, and demonstrates activity against Paclitaxel-resistant A2780T cells[1].
Tubulin polymerization-IN-92 (5 μM; 5 min) inhibits in vitro tubulin polymerization[1].
Tubulin polymerization-IN-92 (10-30 nM; 24 h) disrupts the microtubule network in HT29, A2780S, and A2780T cells[1].
Tubulin polymerization-IN-92 (10-100 nM; 48 h) induces concentration-dependent G2/M phase arrest in HT29 cells[1].
Tubulin polymerization-IN-92 (30-100 nM; 48 h) induces late-stage apoptosis in HeLa cells[1].
Tubulin polymerization-IN-92 (10-100 nM; 14 days) inhibits colony formation in A2780S, A2780T and HT29 cells[1].

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

Tubulin polymerization-IN-92 Related Antibodies

Immunofluorescence[1]

Cell Line: HT29, A2780S, A2780T
Concentration: 10; 30 nM
Incubation Time: 24 h
Result: Induced microtubule depolymerization in HT29, A2780S, and A2780T cells.
Showed intact, organized microtubule networks in untreated cells.

Cell Cycle Analysis[1]

Cell Line: HT29
Concentration: 10, 30, 100 nM
Incubation Time: 48 h
Result: Induced G2/M phase arrest in a concentration-dependent manner.
Increased the proportion of cells in G2/M phase from 8.14% (control) to 60.58% at 100 nM.

Apoptosis Analysis[1]

Cell Line: HeLa
Concentration: 10, 30, 100 nM
Incubation Time: 48 h
Result: Induced late-stage apoptosis in HeLa cells.
Exhibited 8.43% of late apoptotic cells at 30 nM.
Increased late apoptotic cells from 0.47% (control) to 25.12% at 100 nM.

Cell Proliferation Assay[1]

Cell Line: HT29, A2780S, A2780T
Concentration: 40, 100 nM
Incubation Time: 14 days
Result: Significantly decreased the colony number and area of A2780S cells at 40 nM.
Completely inhibited colony formation in A2780T and HT29 cells at 100 nM.
Inhibited colony formation in A2780S
Parmacokinetics
Species Dose Route T1/2 CL AUC0-t Cmax Tmax Vss F
Mice[1] 5 mg/kg i.v. 7.02 h 0.28 L/h/kg 16670.37 μg/L·h 1983.65 μg/L 0.39 h 2.63 L/kg 41.56 %
Mice[1] 10 mg/kg p.o. 6.00 h 0.76 L/h/kg 13856.37 μg/L·h 2139.89 μg/L 0.33 h 6.82 L/kg /
In Vivo

Tubulin polymerization-IN-92 (compound 8h) (5 and 10 mg/kg; p.o.; once daily; 10 days) exhibits antitumor activity in the mouse HT29 xenograft models[1].

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

Animal Model: Female Balb/c mice (5-6 weeks) injected with HT-29 cells[1]
Dosage: 5; 10 mg/kg
Administration: p.o.; once daily; 10 days
Result: Exerted favorable in vivo antitumor activity with tumor growth inhibition (TGI) rates of 58.6% and 70.1% at 5 and
10 mg/kg, respectively.
Showed no significant body weight changes at 5 mg/kg dose.
Exhibited severe toxic side
effect at 10 mg/kg.
Molecular Weight

533.61

Formula

C31H33F2N3O3
SMILES

O=C(NCC1=CC=CC=C1)CC2=C(C=C(C=C2)C3=CC=C(C=C3)OCCN4CCN(CC4)C([C@@H]5C[C@@H]5F)=O)F
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
References
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Tubulin polymerization-IN-92 Related Classifications

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Help & FAQs
  • 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.

Keywords:

Tubulin polymerization-IN-92Microtubule/TubulinApoptosisHCT116A2780THeLapaclitaxel-resistant ovarian cancercolon cancercolchicine siteα-tubulinβ-tubulinA2780Scervical cancerInhibitorinhibitorinhibit

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