WQQ-345
WQQ-345 is an orally active BCAT1 inhibitor with an IC50 values of 10.8 mM. WQQ-345 reduces cellular α-KG levels, upregulating H3K27me3 expression, decreasing glycolytic enzyme expression, and impairing glycolysis activity. WQQ-345 reduces colony formation, suppresses growth of BCAT1-high TKI-resistant lung cancer cells. WQQ-345 exerts in vitro and in vivo antitumor activity. WQQ-345 can be used for the research of TKI-resistant non-small cell lung cancer and TKI-resistant lung cancer.
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- Formule: C10H17NO2
- Masse moléculaire:183.25
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
WQQ-345 (2.5-5 mM; 7-10 days) dose-dependently inhibits colony formation of 67R NSCLC cells[1].
WQQ-345 (5-10 mM; 3 days) dose-dependently reduces intracellular α-KG levels, upregulates H3K27me3 protein expression, and downregulates PFKP and LDHA protein expression in 67R NSCLC cells after 3 days of treatment at 5 mM or 10 mM[1].
WQQ-345 (5 mM; 3 days) impairs glycolytic activity (lowered ECAR) in 67R NSCLC cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ASK120067-resistant NCI-H1975 (67R) NSCLC cells
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Concentration:2.5, 5 mM
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Incubation Time:7-10 days
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Result:Dose-dependently reduced colony formation of 67R cells, with significant inhibition observed at both 2.5 mM and 5 mM.
Resulted in stronger growth inhibition when co-treated with 1 μM ASK120067 (HY-138751) than either monotherapy.
Lost growth-inhibitory effects in 67R cells with BCAT1 knockdown, confirming on-target activity.
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Cell Line:ASK120067-resistant NCI-H1975 (67R) NSCLC cells
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Concentration:5, 10 mM
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Incubation Time:3 days
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Result:Dose-dependently upregulated H3K27me3 protein expression in 67R cells.
Left BCAT1 protein expression unchanged in 67R cells.\n
Dose-dependently reduced protein levels of glycolytic enzymes PFKP and LDHA in 67R cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (4-week-old) subcutaneously injected with 67R cells[1]
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Dosage:80; 120 mg/kg
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Administration:p.o.; twice daily; 43 days
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Result:Achieved robust tumor regression at 120 mg/kg, with significantly smaller tumor volumes compared to vehicle control by day 43.
Increased H3K27me3 protein expression significantly in tumors treated with 120 mg/kg relative to vehicle control tumors.
Decreased protein levels of glycolytic enzymes PFKP, LDHA, and PKM1/2 significantly in tumors treated with 120 mg/kg relative to vehicle control tumors.
Chemical Information
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Masse moléculaire 183.25
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Formule C10H17NO2
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SMILES
O=C(O)C[C@]1(CN)[C@](C2)([H])CC[C@]2([H])C1
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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
[1]. Zhang T, et al. Branched-chain amino acid transaminase 1 confers EGFR-TKI resistance through epigenetic glycolytic activation. Signal Transduct Target Ther. 2024;9(1):216. Published 2024 Aug 15. [Content Brief]
[2]. Luo W, et al. Design, Synthesis and Biological Activity Study of γ-Aminobutyric Acid (GABA) Derivatives Containing Bridged Bicyclic Skeletons as BCAT1 Inhibitors. Molecules. 2025;30(4):904. Published 2025 Feb 15. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
WQQ-345 Related Classifications
HY-169061 Related Classifications
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