Zavondemstat sodium
Zavondemstat (QC8222; TACH 101) sodium is an orally active pan-KDM4 inhibitor, with a IC50 ≤ 0.08 μM against human KDM4A-D and a Kᵢ of 0.52 μM against human KDM4C. Zavondemstat sodium induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat sodium suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat sodium can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer.
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- CAS. Nr.: 2908753-07-9
- Formel: C26H28N3NaO3
- Molecular Weight:453.51
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Zavondemstat (24 h) sodium potently inhibits H3K36me3 demethylation in KYSE-150+KDM4C cells, with an IC50 value of 0.0004 μM in HTRF assays and 0.085 μM in Western blot assays[1].
Zavondemstat (168 h) sodium potently inhibits the proliferation of various cancer cell lines (Jurkat, MDA-MB-231, KYSE-150, MM.1s, HL-60, HT-29, MCF-7, Loucy) with IC50 values ranging from 0.0027 to 0.037 μM, while it exhibits low activity against normal IMR-90 fibroblasts[1].
Zavondemstat (144-168 h) sodium inhibits the viability of SU60, T002C, SU62 colon organoids and PA0165F pancreatic organoids, with IC50 values of < 0.15 μM and < 0.03 μM, respectively, but exhibits low activity against FS53 breast organoids and other non-responsive organoid models[1].
Zavondemstat (72 h) sodium induces apoptosis in KYSE-150, MDA-MB-231 and HT-29 cells, with EC50 values of 0.033, 0.132 and 0.092 μM, respectively[1].
Zavondemstat (0.01-0.1 μM; 48-72 h) sodium induces S-phase cell cycle arrest in MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 (breast cancer cells)
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Concentration:0.01, 0.1 μM
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Incubation Time:48 h, 72 h
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Result:Caused S-phase arrest.
Zavondemstat (12.5-50 mg/kg; p.o.; once daily; for 36 consecutive days) sodium induces dose-dependent tumor growth inhibition in the COH70 triple-negative breast cancer PDX model[1].
Zavondemstat (5-50 mg/kg; p.o.; 3 consecutive days of administration followed by 4 days of withdrawal, or 2 consecutive days of administration followed by 5 days of withdrawal) sodium induces dose-dependent tumor growth inhibition in the GXA-3036 gastric cancer PDX model[1].
Zavondemstat (10-20 mg/kg; p.o.; once daily; for 21 consecutive days) sodium induces dose-dependent tumor growth inhibition in the KYSE-150 esophageal cancer CDX model[1].
Zavondemstat (5-50 mg/kg; p.o.; twice daily, 3 days on/4 days off) sodium induces dose-dependent tumor growth inhibition in the OCI-LY19 DLBCL CDX model[1].
Zavondemstat (40 mg/kg; p.o.; once daily for 21 days) sodium, administered via oral gavage at a dose of 40 mg/kg once daily for 21 days in the SU60 colorectal cancer PDX model, reduces tumorigenic cell populations and decreases the frequency of tumor-initiating cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice (female)[1]
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Dosage:10 mg/kg; 20 mg/kg; 10 mg/kg (3 days on/4 days off); 10 mg/kg (5 days on/2 days off)
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Administration:p.o.; once daily; 7 days; 3 days on/4 days off; 5 days on/2 days off
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Result:Observed dose-dependent tumor growth inhibition (TGI): achieved 48% TGI at 10 mg/kg daily for 7 days, 71% TGI at 20 mg/kg daily for 7 days, 52% TGI at 10 mg/kg 3 days on/4 days off, and 42% TGI at 10 mg/kg 5 days on/2 days off.
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Animal Model:NSG mice (female)[1]
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Dosage:12.5 mg/kg; 25 mg/kg; 40 mg/kg; 50 mg/kg
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Administration:p.o.; once daily; 36 days
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Result:Observed dose-dependent tumor growth inhibition (TGI): achieved 57% TGI at 12.5 mg/kg, 68% TGI at 25 mg/kg, 86% TGI at 40 mg/kg, and 86% TGI at 50 mg/kg.
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Animal Model:NSG mice[1]
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Dosage:5 mg/kg; 15 mg/kg; 22.5 mg/kg; 50 mg/kg
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Administration:p.o.; 3 days on/4 days off; 2 days on/5 days off
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Result:Observed dose-dependent tumor growth inhibition (TGI): achieved 43% TGI at 5 mg/kg, 69% TGI at 15 mg/kg, 52% TGI at 50 mg/kg, and 41% TGI at 22.5 mg/kg
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Animal Model:NSG mice[1]
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Dosage:10 mg/kg; 15 mg/kg; 20 mg/kg
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Administration:p.o.; once daily; 21 days
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Result:Observed dose-dependent tumor growth inhibition (TGI): achieved 54% TGI at 10 mg/kg, 76% TGI at 15 mg/kg, and 84% TGI at 20 mg/kg.
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Animal Model:NSG mice[1]
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Dosage:5 mg/kg; 15 mg/kg; 50 mg/kg; 25 mg/kg (twice daily)
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Administration:p.o.; 3 days on/4 days off; twice daily (25 mg/kg group)
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Result:Observed dose-dependent tumor growth inhibition (TGI): achieved 55% TGI at 5 mg/kg, 83% TGI at 15 mg/kg, 90% TGI at 50 mg/kg, and 102% TGI (with three of eight complete remissions) at 25 mg/kg twice daily.
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Animal Model:NSG mice (female)[1]
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Dosage:40 mg/kg
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Administration:p.o.; daily; 21 days
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Result:Reduced the proportion of tumorigenic CD44HighEpCAM+ cells by 2.5-fold and reduced tumor-initiating cell frequency by 4.4-fold compared to vehicle.
Chemical Information
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CAS. Nr. 2908753-07-9
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Molecular Weight 453.51
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Formel C26H28N3NaO3
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SMILES
O=C(O[Na])C1=CC=NC=C1NC[C@H]2C3=CC=C(N(C4=CC=C(C=C4)C(C)C)C)C=C3OCC2
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Synonyms
QC8222 sodium; TACH 101 sodium
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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
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Zavondemstat sodium Related Classifications
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