Antitumor agent-234
Antitumor agent-234 is an orally active antitumor agent. Antitumor agent-234 inhibits EGFR phosphorylation and downstream MAPK signaling, reduces the phosphorylation and activation levels of RAF and MEK, and induces DNA damage, S-phase cell cycle arrest, and Apoptosis. Antitumor agent-234 inhibits Ki67 expression. Antitumor agent-234 exerts anticancer effects against esophageal squamous cell carcinoma.
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- CAS. Nr.: 2699021-56-0
- Formel: C35H42F3N3O11
- Molecular Weight:737.72
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
Antitumor agent-234 is an orally active antitumor agent. Antitumor agent-234 inhibits EGFR phosphorylation and downstream MAPK signaling, reduces the phosphorylation and activation levels of RAF and MEK, and induces DNA damage, S-phase cell cycle arrest, and Apoptosis. Antitumor agent-234 inhibits Ki67 expression. Antitumor agent-234 exerts anticancer effects against esophageal squamous cell carcinoma[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KYSE-150 cell line | IC50 |
0.126 mM
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Antiproliferative activity against human KYSE150 esophageal cancer cells assessed as viability reduction after 48 hrs by MTT assay.
Antiproliferative activity against human KYSE150 esophageal cancer cells assessed as viability reduction after 48 hrs by MTT assay.
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42648056 |
| KYSE-520 cell line | IC50 |
0.003 mM
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Antiproliferative activity against human KYSE520 esophageal cancer cells assessed as viability reduction after 48 hrs by MTT assay.
Antiproliferative activity against human KYSE520 esophageal cancer cells assessed as viability reduction after 48 hrs by MTT assay.
|
42648056 |
| ECa-109 cell line | IC50 |
0.051 mM
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Antiproliferative activity against human Eca109 esophageal cancer cells assessed as viability reduction after 48 hrs by MTT assay.
Antiproliferative activity against human Eca109 esophageal cancer cells assessed as viability reduction after 48 hrs by MTT assay.
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42648056 |
In Vitro
Anti-cancerApoptosisCell Cycle Regulation
Anti-cancer
Antitumor agent-234 (Compound GD1) (48 h) inhibits proliferation of KYSE150, KYSE520, and Eca109 esophageal cancer cells, with IC50 values of 0.126, 0.003, and 0.051 mM, respectively[1].
Antitumor agent-234 (128 μM; 48 h) induces DNA damage in KYSE150 cells, evidenced by comet-tail formation[1].
Antitumor agent-234 (128 μM; 48 h) upregulates γ-H2AX in KYSE150 cells, consistent with DNA double-strand break induction[1].
Antitumor agent-234 (128 μM; 48 h) upregulates Cyclin A without appreciably affecting Cyclin D1 or Cyclin E1 in KYSE150 cells[1].
Antitumor agent-234 (128 μM; 48 h) suppresses EGFR/MAPK pathway phosphorylation in KYSE150 cells[1].
Antitumor agent-234 (128 μM; 48 h) induces DNA damage in KYSE150 cells, evidenced by comet-tail formation[1].
Antitumor agent-234 (128 μM; 48 h) upregulates γ-H2AX in KYSE150 cells, consistent with DNA double-strand break induction[1].
Antitumor agent-234 (128 μM; 48 h) upregulates Cyclin A without appreciably affecting Cyclin D1 or Cyclin E1 in KYSE150 cells[1].
Antitumor agent-234 (128 μM; 48 h) suppresses EGFR/MAPK pathway phosphorylation in KYSE150 cells[1].
Anti-cancer
Apoptosis
Antitumor agent-234 (128 μM; 48 h) induces apoptosis in KYSE150 and KYSE520 esophageal cancer cells, with the KYSE150 Annexin V-FITC/PI profile showing Q2 3.32% and Q3 33.2%[1].
Antitumor agent-234 (128 μM; 48 h) shifts KYSE150 and KYSE520 cells toward mitochondrial apoptosis by increasing Bax/Bcl-2 and activating caspase-3/7[1].
Antitumor agent-234 (128 μM; 48 h) shifts KYSE150 and KYSE520 cells toward mitochondrial apoptosis by increasing Bax/Bcl-2 and activating caspase-3/7[1].
Anti-cancer
Cell Cycle Regulation
Antitumor agent-234 (128 μM; 48 h) increases the S-phase fraction in KYSE150 cells to 41.3%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis[1]
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Cell Line:KYSE150 human esophageal cancer cells
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Concentration:128 μM
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Incubation Time:48 h
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Result:γ-H2AX expression was significantly increased compared with control.\nNo appreciable effect on Cyclin D1 or Cyclin E1 expression was observed, while Cyclin A was pronouncedly upregulated.\nPhosphorylation levels of EGFR, Raf, Mek1/2, and Erk were reduced.
Cell Cycle Analysis[1]
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Cell Line:KYSE150 human esophageal cancer cells
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Concentration:128 μM
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Incubation Time:48 h
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Result:G1 was 58.5%, S was 41.3%, and G2 was 0.76%.
Apoptosis Analysis[1]
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Cell Line:KYSE150 and KYSE520 human esophageal cancer cell lines
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Concentration:128 μM
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Incubation Time:48 h
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Result:Induced apoptosis in KYSE150 and KYSE520 cells, with the most pronounced pro-apoptotic effect among the groups.
In the supplied KYSE150 flow plot, Q2 was 3.32% and Q3 was 33.2%.
Western Blot Analysis[1]
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Cell Line:KYSE150 and KYSE520 human esophageal cancer cell lines
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Concentration:128 μM
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Incubation Time:48 h
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Result:Significantly upregulated Bax and downregulated Bcl-2, increasing the Bax/Bcl-2 ratio.
Cleaved caspase-3 and cleaved caspase-7 levels were increased, and pro-caspase-3 and pro-caspase-7 levels were decreased in both KYSE150 and KYSE520 cells.
In Vivo
Anti-cancer
Antitumor agent-234 (500 mg/kg; p.o. and i.p.; twice weekly for 2 weeks) inhibited AsPC-1 xenograft tumor growth by 51.35% in nude mice[1].
Antitumor agent-234 (5-10 mg/kg; p.o.; five consecutive days per week for 3 weeks) inhibited KYSE150 xenograft tumor growth by 86.96% in nude mice[1].
Antitumor agent-234 (10 mg/kg; p.o.; five consecutive days per week for 3 weeks) inhibited Eca109 xenograft tumor growth by 70.40% in nude mice[1].
Antitumor agent-234 (5-10 mg/kg; p.o.; five consecutive days per week for 3 weeks) inhibited KYSE150 xenograft tumor growth by 86.96% in nude mice[1].
Antitumor agent-234 (10 mg/kg; p.o.; five consecutive days per week for 3 weeks) inhibited Eca109 xenograft tumor growth by 70.40% in nude mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-nu (nude) (female, 8 weeks old, 18-22 g)[1]
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Dosage:500 mg/kg (p.o.); 500 mg/kg (i.p.)
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Administration:p.o. and i.p.; twice weekly for 2 weeks
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Result:At 500 mg/kg p.o., tumor weight was 0.18 g and tumor inhibitory rate was 51.35%.
At 500 mg/kg i.p., tumor weight was 0.18 g and tumor inhibitory rate was 51.35%.
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Animal Model:BALB/c-nu (nude) (female, 8 weeks old, 18-22 g)[1]
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Dosage:5 mg/kg (p.o.); 7.5 mg/kg (p.o.); 10 mg/kg (p.o.)
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Administration:p.o.; five consecutive days per week for 3 weeks
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Result:Dose-dependent tumor growth inhibition was observed.
At 10 mg/kg, tumor inhibitory rate was 86.96%.
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Animal Model:BALB/c-nu (nude) (female, 8 weeks old, 18-22 g)[1]
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Dosage:10 mg/kg (p.o.)
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Administration:p.o.; five consecutive days per week for 3 weeks
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Result:At 10 mg/kg, tumor growth was significantly suppressed compared with control, with a tumor inhibitory rate of 70.40%.
Related Protocols :
- Western Blot
- RNA extraction experimental
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Protocol for Cell Cycle
- Kinase activity and phosphorylation assays
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Ki-67 Immunostaining Proliferation Assay
- Flow cytometric DNA-content cell-cycle staining
- Apoptosis Solutions
- Protocol for Kinase activity and phosphorylation assays
- Genotoxicity/Mutagenicity Study
Chemical Information
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CAS. Nr. 2699021-56-0
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Molecular Weight 737.72
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Formel C35H42F3N3O11
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SMILES
FC1(F)[C@H](O)[C@@H](CO)O[C@H]1N(C=C2)C(N=C2NC(CCC(OCC([C@@]3(O)[C@H](C)C[C@]4([H])[C@]3(C)C[C@@H]([C@@]5([C@]6(C=CC(C=C6CC[C@@]45[H])=O)C)F)O)=O)=O)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Select Batch:
Reinheit:
99.98%
Assay:
99.98%
ee.:
99.98%
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Calculators
Molaritätsrechner
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
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Verdünnungsrechner
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Antitumor agent-234 Related Classifications
HY-190668 Related Classifications
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Keywords
- Antitumor agent-234
- 2699021-56-0
- Antitumor agent234
- Antitumor agent 234
- EGFR
- p38 MAPK
- Raf
- MEK
- DNA/RNA Synthesis
- Apoptosis
- Epidermal growth factor receptor
- ErbB-1
- HER1
- Raf kinases
- Mitogen-activated protein kinase kinase
- MAPKK
- MAP2K
- DNA damage
- MAPK signaling
- RAF
- S-phase cell cycle arrest
- esophageal squamous carcinoma
- mitochondrial apoptosis
- proliferation
- xenograft
- Inhibitor
- inhibitor
- inhibit