Zavondemstat L-lysine  (Synonyms: QC8222; TACH 101)

Zavondemstat (QC8222; TACH 101) L-lysine 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 L-lysine induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat L-lysine suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat L-lysine can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer^[1].

Zavondemstat (24 h) L-lysine 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) L-lysine 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) L-lysine 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) L-lysine 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) L-lysine 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.

Zavondemstat (10-20 mg/kg; p.o.; daily administration with schedules of 3 days on/4 days off and 5 days on/2 days off; for a total of 7 days) L-lysine induces dose-dependent tumor growth inhibition in the SU60 colorectal cancer PDX model^[1].
Zavondemstat (12.5-50 mg/kg; p.o.; once daily; for 36 consecutive days) L-lysine 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) L-lysine 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) L-lysine 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) L-lysine 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) L-lysine, 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.

577.71

C₃₂H₄₃N₅O₅

2908753-10-4

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Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Chandhasin C, et al. TACH101, a first-in-class pan-inhibitor of KDM4 histone demethylase. Anticancer Drugs. 2023;34(10):1122-1131.  [Content Brief]