2. Epigenetics Apoptosis
  3. Histone Demethylase Apoptosis
  4. Zavondemstat

Zavondemstat  (Synonyms: QC8222 free base; TACH 101 free base)

Cat. No.: HY-148807 Purity: 99.29% ee.: 100.00%
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Zavondemstat (QC8222 free base; TACH 101 free base) 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 induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer.

For research use only. We do not sell to patients.

Zavondemstat

Zavondemstat Chemical Structure

CAS No. : 1851412-93-5

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Based on 1 publication(s) in Google Scholar

Other Forms of Zavondemstat:

Zavondemstat Related Antibodies

Top Publications Citing Use of Products

View All Histone Demethylase Isoform Specific Products:

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target[1]

KDM4A

≤ 0.08 μM (IC50)

KDM4B

≤ 0.08 μM (IC50)

KDM4C

≤ 0.08 μM (IC50)

KDM4D

≤ 0.08 μM (IC50)

In Vitro

Zavondemstat (24 h) 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) 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) 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) 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) 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 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 (breast cancer cells)
Concentration: 0.01, 0.1 μM
Incubation Time: 48 h, 72 h
Result: Caused S-phase arrest.
In Vivo

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) 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) 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) 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) 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) 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), 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.

Animal Model: NSG mice (female)[1]
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)
Administration: p.o.; once daily; 7 days; 3 days on/4 days off; 5 days on/2 days off
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.
Animal Model: NSG mice[1]
Dosage: 12.5 mg/kg; 25 mg/kg; 40 mg/kg; 50 mg/kg
Administration: p.o.; once daily; 36 days
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.
Animal Model: NSG mice[1]
Dosage: 5 mg/kg; 15 mg/kg; 22.5 mg/kg; 50 mg/kg
Administration: p.o.; 3 days on/4 days off; 2 days on/5 days off
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
Animal Model: NSG mice[1]
Dosage: 10 mg/kg; 15 mg/kg; 20 mg/kg
Administration: p.o.; once daily; 21 days
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.
Animal Model: NSG mice[1]
Dosage: 5 mg/kg; 15 mg/kg; 50 mg/kg; 25 mg/kg (twice daily)
Administration: p.o.; 3 days on/4 days off; twice daily (25 mg/kg group)
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.
Animal Model: NSG mice (female)[1]
Dosage: 40 mg/kg
Administration: p.o.; daily; 21 days
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.
Molecular Weight

431.53

Formula

C26H29N3O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

OC(C1=CC=NC=C1NC[C@H]2C3=CC=C(N(C4=CC=C(C=C4)C(C)C)C)C=C3OCC2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMF : 10 mg/mL (23.17 mM; Need ultrasonic)

DMSO : 4.17 mg/mL (9.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3173 mL 11.5867 mL 23.1734 mL
5 mM 0.4635 mL 2.3173 mL 4.6347 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMF    90% Corn Oil

    Solubility: ≥ 1 mg/mL (2.32 mM); Clear solution

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.29% ee.: 100.00%

SDS (252 KB)

COA (248 KB) HNMR (305 KB) NP-HPLC (244 KB) LCMS (103 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / DMF 1 mM 2.3173 mL 11.5867 mL 23.1734 mL 57.9334 mL
5 mM 0.4635 mL 2.3173 mL 4.6347 mL 11.5867 mL
DMF 10 mM 0.2317 mL 1.1587 mL 2.3173 mL 5.7933 mL
15 mM 0.1545 mL 0.7724 mL 1.5449 mL 3.8622 mL
20 mM 0.1159 mL 0.5793 mL 1.1587 mL 2.8967 mL
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Zavondemstat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Zavondemstat1851412-93-5QC8222TACH 101QC 8222QC-8222TACH101TACH-101Histone DemethylaseApoptosisKDM4DKDM4AKDM4CS-phase cell cycle arresthistone H3K9me3KDM4Bapoptosiscolorectal cancerhistone H3K36me3alpha-ketoglutarateInhibitorinhibitorinhibit

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