TXX-1-10
TXX-1-10 is a HPIP inhibitor. TXX-1-10 reduces HPIP expression and disrupts the formation of the EGFR-RAS-ERK signaling complex. TXX-1-10 inhibits AKT and ERK1/2 phosphorylation/activation and inhibits FAK and paxillin phosphorylation. TXX-1-10 induces G1 cell cycle arrest and apoptosis, and inhibits cancer cell proliferation, migration, invasion, epithelial-mesenchymal transition, and tumor growth/metastasis. TXX-1-10 can be used for research on breast cancer and lung cancer.
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- CAS No.: 2489250-48-6
- Formule: C23H18Cl3IN4O
- Masse moléculaire:599.68
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Stockage:
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]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
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HPIP |
EGFR |
Ras |
ERK1 |
ERK2 |
Akt |
FAK |
paxillin |
In Vitro
TXX-1-10 (48 h) reduces cancer cell viability with IC50 values of 2.2-7.9 µM and inhibits the proliferation and colony formation of MDA-MB-231 and ZR-751 cells[1].
TXX-1-10 (1-10 µM; migration 0-12 h; invasion 24 h) inhibits the migration and invasion of ZR-751 and MDA-MB-231 cells[1].
TXX-1-10 (24 h) inhibits FAK and paxillin phosphorylation in ZR75-1 and MDA-MB-231 cells and reverses EMT marker expression[1].
TXX-1-10 broadly modulates the expression of genes related to DNA replication, cell cycle, apoptosis, adhesion, and migration/invasion in MDA-MB-231 cells, including genes regulated by HPIP[1].
TXX-1-10 reduces HPIP expression in A549 and ZR75-1 cancer cells and decreases the interactions among components of the EGFR-RAS-ERK pathway[2].
TXX-1-10 (10 μM; 24 h) inhibits the activation of the EGFR-RAS-ERK signaling pathway in A549 and ZR75-1 cancer cells[2].
TXX-1-10 inhibits the proliferation of A549, ZR75-1, and Calu-3 cancer cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ZR-751 and MDA-MB-231 cells
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Concentration:1, 5, 10 µM
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Incubation Time:0 and 12 h (migration); 24 h (invasion)
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Result:Wound-healing assay and matrigel invasion assay showed that TXX-1-10 specifically inhibited the migration and invasion of ZR-751 and MDA-MB-231 cells in a dose-dependent manner.
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Cell Line:A549 lung cancer and ZR75-1 breast cancer cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Abrogated the ability of EGFR, GRB2, KRAS, or RAF1 overexpression to stimulate GTP-bound RAS level, RAF1, MEK1/2, and ERK1/2 phosphorylation, and c-Myc, HIF-1α, and c-Fos expression; these effects were reversed by HPIP overexpression.
In Vivo
TXX-1-10 (30 mg/kg; intraperitoneal injection) inhibits tumor growth in the ZR75-1 breast cancer xenograft model[2].
TXX-1-10 (30 mg/kg; intraperitoneal injection) inhibits tumor growth in the A549 lung cancer xenograft model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:nude (BALB/c background; female; 6 weeks old)[1]
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Dosage:30 mg/kg
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Administration:i.p.; ~20 days
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Result:Compared to the Rimonabant (HY-14136) groups, the TXX-1-10 groups showed a more significant inhibitory effect on the amount of Ki67 (proliferation marker)-, CD31 (endothelial cell marker)-, and HPIP-positive tumor cells, and a more significant stimulatory effect on the amount of cleaved caspase-3 (apoptosis marker)-positive tumor cells.
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Animal Model:nude (BALB/c)[1]
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Dosage:30 mg/kg
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Administration:i.p.
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Result:The lung metastasis of the TXX-1-10 group was significantly decreased compared with that of the Rimonabant group.
Survival rates of the TXX-1-10 groups were higher than those of the Rimonabant groups.
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Animal Model:BALB/c nude (female, 6 weeks old)[2]
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Dosage:30 mg/kg
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Administration:i.p.
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Result:Inhibited tumor growth in the ZR75-1 breast cancer xenograft, with effects similar to HPIP knockout in KRAS- and MEK1-overexpressing tumors.
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Animal Model:nude (6 weeks old)[2]
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Dosage:30 mg/kg
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Administration:i.p.
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Result:Inhibited tumor growth in the A549 lung cancer xenograft, with effects similar to HPIP knockout in KRAS- and MEK1-overexpressing tumors.
- RNA extraction experimental
- Cell migration
- Somatic Cell Culture
- Breast Cancer Modeling
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Apoptosis Solutions
- Cell invasion
- MTT Cell Proliferation Assay
- Western Blot
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Cell Cycle
- CCK-8/WST-8 Cell Proliferation Assay
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Protocol for Kinase activity and phosphorylation assays
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
Chemical Information
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CAS No. 2489250-48-6
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Masse moléculaire 599.68
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Formule C23H18Cl3IN4O
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SMILES
CC1=C(C2=CC=C(Cl)C=C2)N(C3=CC=C(Cl)C=C3Cl)N=C1C(NC4=CC=C[N+](C)=C4)=O.[I-]
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TXX-1-10 Related Classifications
HY-188268 Related Classifications
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Keywords
- TXX-1-10
- 2489250-48-6
- EGFR
- Ras
- ERK
- Akt
- FAK
- Apoptosis
- Epidermal growth factor receptor
- ErbB-1
- HER1
- Extracellular signal regulated kinases
- PKB
- Protein kinase B
- PTK2 protein tyrosine kinase 2
- PTK2
- Focal adhesion kinase
- AKT
- ALDH1
- EGFR-RAS-ERK signaling
- ERK1/2
- ERα
- G1 cell cycle arrest
- HPIP
- RAS
- aerobic glycolysis
- apoptosis
- blood-brain barrier permeability
- breast cancer
- cancer cell proliferation
- cancer stem cell
- cathepsin D
- epithelial-to-mesenchymal transition
- invasion
- lung cancer
- metastasis
- migration
- oxidative respiration
- pS2
- paxillin
- tumor growth
- Inhibitor
- inhibitor
- inhibit