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.
- Formula: C24H19ClN2O4S
- Molecular Weight:466.94
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All EGFR Isoforms
More
Biological Activity
|
EGFR |
Akt |
Ras |
mTOR |
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.
-
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.
-
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 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.
-
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.
-
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).
-
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.
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.
Chemical Information
-
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
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tubulin-IN-64 Related Classifications
HY-181491 Related Classifications
Powered by Bioz
- Tubulin-IN-64
- Microtubule/Tubulin
- EGFR
- Akt
- mTOR
- Ras
- Apoptosis
- Autophagy
- Aitumor activity
- sulfonated styrylquinazoline derivative
- GFR/Akt/mTOR and EGFR/Ras signaling inhibitor
- microtubule polymerization promoter
- cell cycle arrest inducer
- apoptosis inducer
- autophagy inducer
- glioblastoma (GBM)
- leukemia
- U87MG cells
- U-251 cells
- K562 cells
- NHA cells
- HepG2 cells
- zebrafish GBM xenograft model
- Inhibitor
- inhibitor
- inhibit