2. Cell Cycle/DNA Damage Cytoskeleton Protein Tyrosine Kinase/RTK JAK/STAT Signaling PI3K/Akt/mTOR MAPK/ERK Pathway GPCR/G Protein Apoptosis Autophagy
  3. Microtubule/Tubulin EGFR Akt mTOR Ras Apoptosis Autophagy
  4. Tubulin-IN-64

Tubulin-IN-64 is a sulfonated styrylquinazoline derivative with high selectivity antitumor activity. Tubulin-IN-64 targets tubulin, inhibits the EGFR/Akt/mTOR and EGFR/Ras signaling pathways, induces cell cycle arrest, apoptosis and autophagy. Tubulin-IN-64 exhibits significant antitumor efficacy in the zebrafish GBM xenograft model. Tubulin-IN-64 can be used for the research on glioblastoma and leukemia.

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

Tubulin-IN-64

Tubulin-IN-64 Chemical Structure

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Tubulin-IN-64 Related Antibodies

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  • Biological Activity

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Description

Tubulin-IN-64 is a sulfonated styrylquinazoline derivative with high selectivity antitumor activity. Tubulin-IN-64 targets tubulin, inhibits the EGFR/Akt/mTOR and EGFR/Ras signaling pathways, induces cell cycle arrest, apoptosis and autophagy. Tubulin-IN-64 exhibits significant antitumor efficacy in the zebrafish GBM xenograft model. Tubulin-IN-64 can be used for the research on glioblastoma and leukemia[1].

IC50 & Target[1]

EGFR

 

Akt

 

Ras

 

mTOR

 

In Vitro

Tubulin-IN-64 (TS5) (72 h) exhibits potent antiproliferative activity against human glioblastoma U87MG (IC50 = 0.17 μM), U-251 (IC50 = 0.21 μM) and human chronic myelogenous leukemia K562 cells (IC50 = 0.26 M), with negligible cytotoxicity to human hepatoma HepG2 cells (IC50 > 25 μM), moderate antiproliferative activity against normal human astrocytes (NHA) (IC50 = 1.75 μM) [1].
Tubulin-IN-64 (10 μM; 90 min) significantly promotes tubulin polymerization in the in vitro tubulin polymerization assay [1]. Tubulin-IN-64 (0.63 μM; 3 h) disrupts microtubule assembly-disassembly dynamics and induces a disordered and condensed microtubule cytoskeleton in U-251 cells[1].
Tubulin-IN-64 (1.3 μM; 48 h) induces significant apoptosis in K562 cells, with around 50% of the cells in early and late apoptotic[1].
Tubulin-IN-64 (0.4 μM; 24 h) induces G2/M phase cell cycle arrest in U-251 cells, downregulates EGFR (Tyr1068), Akt (Ser473), mTOR (Ser2448) and STAT5 phosphorylation, and upregulates cell cycle-related proteins (p27, p21, cyclin B1, cdc2, Aurora A) and pro-apoptotic proteins (cleaved caspase-9, cleaved PARP-1, BID) in U-251 cells[1].
Tubulin-IN-64 (1.3 μM; 24 h) triggers G2/M phase cell cycle arrest in K562 cells, downregulates EGFR (Tyr1068), Akt (Ser473), mTOR (Ser2448) and STAT5 phosphorylation, and upregulates cell cycle-related proteins (p27, p21, cyclin B1, cdc2, Aurora A) and pro-apoptotic proteins (cleaved caspase-9, cleaved PARP-1, BID) in K5[1].

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

Tubulin-IN-64 Related Antibodies

Cell Autophagy Assay[1]

Cell Line: U-251 cells and K562 cells
Concentration: 0.4 μM and 1.3 μM
Incubation Time: 24 h
Result: Apoptosis was the main mode of cell death in U-251 (no significant autophagy gene changes); in K562, upregulated autophagy-related genes (calreticulin, LC3), indicating autophagy involvement in p53-deficient cell death.

RT-PCR[1]

Cell Line: U-251 cells and K562 cells
Concentration: 0.4 μM and 1.3 μM
Incubation Time: 24 h
Result: Downregulated CCNE2 and IDH1 (U-251) or CCNE2 (K562, 5.8-fold decrease) mRNA expression.
Upregulated GADD45 in both cell lines, and additionally upregulated TUBB3 (> 2.2-fold), calreticulin and LC3 in K562 cells.

Cell Cycle Analysis[1]

Cell Line: U-251 cells and K562 cells
Concentration: 0.4 μM and 1.3 μM
Incubation Time: 24 h
Result: Caused significant G2/M phase cell cycle arrest.

Immunofluorescence[1]

Cell Line: U-251 cells
Concentration: 0.63 μM
Incubation Time: 3 h
Result: Disrupted microtubule polymerization-depolymerization dynamics and induced a disordered microtubule cytoskeletal network.

Western Blot Analysis[1]

Cell Line: U-251 cells and K562 cells
Concentration: 0.4 μM and 1.3 μM
Incubation Time: 24 h
Result: Upregulated the expression of cell cycle-related proteins (p27, p21, cyclin B1, cdc2, Aurora A) and pro-apoptotic proteins (cleaved caspase-9, cleaved PARP-1, BID).
Downregulated the phosphorylation of EGFR (Tyr1068), mTOR (Ser2448) (U-251) or Akt (Ser473), STAT5 (Tyr694) and RAS expression (K562).

Apoptosis Analysis[1]

Cell Line: U-251 cells and K562 cells
Concentration: 0.2/0.4 μM and 1.3 μM
Incubation Time: 48 h
Result: Induced significant apoptosis: nearly 75% of U-251 cells and around 50% of K562 cells underwent early and late apoptosis.
In Vivo

Tubulin-IN-64 (TS5) (0.5-2 μM; immersion; 72 h) exhibits dose-dependent antitumor activity in zebrafish GBM xenograft models implanted with U-251 cells, with the 2 μM dose showing more potent efficacy than osimertinib (10 μM)[1].
Tubulin-IN-64 (1-5 μM; immersion; 96 h) has acute toxicity in zebrafish embryos with an LC₅₀ value of 3.614 μM, and at concentrations ≥ 3 μM, it induces dose-dependent cardiotoxicity and developmental malformations (scoliosis, pericardial edema, abdominal opacity in zebrafish larvae[1].

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

Animal Model: Female and male immunocompetent zebrafish embryos (freshly obtained) were used for acute toxicity assay[1].
Dosage: 1, 2, 3, 4, 5 μM
Administration: Immersion, continuous exposure; 96 h
Result: Exhibited acute toxicity with a median LC50 of 3.614 μM.
Induced developmental endpoints including embryo coagulation, absence of somite formation, tail separation disorder and lack of cardiac activity at concentrations up to 15 μM.
Showed dose-dependent cardiotoxic potential, with noticeable reduction in heart rate (beats per minute) compared to the control group.
Induced developmental malformations including scoliosis (body-axis curvature), pericardial edema and abdominal opacity, with severity and frequency increasing.
Animal Model: Female and male immunocompetent zebrafish embryos (2 days post-fertilization, 2-dpf) were intra-yolk sac injected with human glioblastoma U-251 cells (500-1000 fluorescently labeled cells per embryo[1].
Dosage: 0.5, 1, 2 μM
Administration: Immersion, continuous exposure; 72 h
Result: Demonstrated dose-dependent antitumor efficacy.
Significantly inhibited tumor growth, quantified by reduced tumor-derived fluorescence at the injection site.
Exhibited sublethal effects without causing severe developmental abnormalities at the tested concentrations.
Molecular Weight

466.94

Formula

C24H19ClN2O4S
SMILES

O=S(C1=CC=C(C)C=C1)(OC2=C3C=C(Cl)C=CC3=NC(/C=C/C4=CC=CC=C4OC)=N2)=O
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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-IN-64 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-IN-64Microtubule/TubulinEGFRAktmTORRasApoptosisAutophagyEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BMammalian target of RapamycinAitumor activitysulfonated styrylquinazoline derivativeGFR/Akt/mTOR and EGFR/Ras signaling inhibitormicrotubule polymerization promotercell cycle arrest inducerapoptosis inducerautophagy inducerglioblastoma (GBM)leukemiaU87MG cellsU-251 cellsK562 cellsNHA cellsHepG2 cellszebrafish GBM xenograft modelInhibitorinhibitorinhibit

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