| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Zavondemstat (24 h) sodium effectively inhibited the demethylation of H3K36me3 in KYSE-150+KDM4C cells, with an IC50 value of 0.0004 μM in HTRF assay and 0.085 μM in Western blot assay [1]. Zavondemstat (168 h) sodium effectively inhibited the proliferation of various cancer cell lines (Jurkat, MDA-MB-231, KYSE-150, MM.1s, HL-60, HT-29, MCF-7, Loucy), with an IC50 value ranging from 0.0027 to 0.037 μM, while its activity against normal IMR-90 fibroblasts was low [1]. Zavondemstat sodium (144-168 h) inhibited the activity of SU60, T002C, SU62 colon organoids and PA0165F pancreatic organoids, with IC50 values of < 0.15 μM and < 0.03 μM, respectively, but had low activity against FS53 mammary organoids and other unresponsive organoid models [1]. Zavondemstat sodium (72 h) induced 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 sodium (0.01-0.1 μM; 48-72 h) induced S-phase cell cycle arrest in MDA-MB-231 cells [1].
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| ln Vivo |
Zavondemstat sodium (10-20 mg/kg; orally; daily, with a dosing regimen of 3 days on, 4 days off or 5 days on, 2 days off for a total of 7 days) induced dose-dependent tumor growth inhibition in the SU60 colorectal cancer PDX model [1]. Zavondemstat sodium (12.5-50 mg/kg; orally; once daily for 36 days) induced dose-dependent tumor growth inhibition in the COH70 triple-negative breast cancer PDX model [1]. Zavondemstat sodium (5-50 mg/kg; orally; 3 days on, 4 days off, or 2 days on, 5 days off) induced dose-dependent tumor growth inhibition in the GXA-3036 gastric cancer PDX model [1]. In the KYSE-150 esophageal cancer CDX model, Zavondemstat sodium (10-20 mg/kg; orally; once daily for 21 days) induced dose-dependent tumor growth inhibition [1]. In the OCI-LY19 diffuse large B-cell lymphoma CDX model, Zavondemstat sodium (5-50 mg/kg; orally; twice daily for 3 days followed by 4 days off) induced dose-dependent tumor growth inhibition [1]. In the SU60 colorectal cancer PDX model, Zavondemstat sodium (40 mg/kg; orally; once daily for 21 days) administered by gavage at a dose of 40 mg/kg once daily reduced the number of tumorigenic cells and decreased the frequency of tumor-initiating cells [1].
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| Animal Protocol |
Animal/Disease Models:NSG Mice (Female) [1]
Doses: 10 mg/kg; 20 mg/kg; 10 mg/kg (3 days on, 4 days off); 10 mg/kg (5 days on, 2 days off) Route of Administration: Oral; once daily; for 7 consecutive days; 3 days on, 4 days off; 5 days on, 2 days off Experimental Experimental Results: Dose-dependent tumor growth inhibition (TGI) was observed: 48% for 10 mg/kg daily for 7 consecutive days; 71% for 20 mg/kg daily for 7 consecutive days; 52% for 10 mg/kg daily for 3 days on, 4 days off; and 42% for 10 mg/kg daily for 5 days on, 2 days off. Animal/Disease Models:NSG Mice (Female) [1] Doses: 12.5 mg/kg; 25 mg/kg; 40 mg/kg; 50 mg/kg Route of Administration: Oral; once daily; 36 days Experimental Results: Dose-dependent tumor growth inhibition (TGI) was observed: 57% at 12.5 mg/kg, 68% at 25 mg/kg, 86% at 40 mg/kg, and 86% at 50 mg/kg. Animal/Disease Models:NSG Mice [1] Doses: 5 mg/kg; 15 mg/kg; 22.5 mg/kg; 50 mg/kg Route of Administration: Oral; 3 days of continuous administration/4 days off; 2 days of continuous administration/5 days off Experimental Results: Dose-dependent tumor growth inhibition rate (TGI) was observed: 43% at 5 mg/kg, 69% at 15 mg/kg, 52% at 50 mg/kg, and 41% at 22.5 mg/kg. Animal/Disease Models:NSG Mice [1] Doses: 10 mg/kg; 15 mg/kg; 20 mg/kg Route of Administration: Oral; once daily; 21 days Experimental Results: Dose-dependent tumor growth inhibition (TGI) was observed: 54% at 10 mg/kg, 76% at 15 mg/kg, and 84% at 20 mg/kg. Animal/Disease Models:NSG Mice [1] Doses: 5 mg/kg; 15 mg/kg; 50 mg/kg; 25 mg/kg (twice daily) Route of Administration: Oral; 3 days on/4 days off; twice daily (25 mg/kg group) Experimental Results: Dose-dependent tumor growth inhibition (TGI) was observed: 55% at 5 mg/kg, 83% at 15 mg/kg, 90% at 50 mg/kg, and 102% at 25 mg/kg twice daily (3 out of 8 cases achieved complete remission). Animal/Disease Models:NSG Mice (Female) [1] Doses: 40 mg/kg Route of Administration: Oral; Daily; 21 days Experimental Results: Compared with the vector, the proportion of tumorigenic CD44HighEpCAM+ cells was reduced by 2.5 times and the frequency of tumor-initiating cells was reduced by 4.4 times. |
| References |
| Molecular Formula |
C26H28N3NAO3
|
|---|---|
| Molecular Weight |
453.51
|
| CAS # |
2908753-07-9
|
| Appearance |
Typically exists as solids at room temperature
|
| 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
|
| Synonyms |
QC8222 sodium; TACH 101 sodium
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2050 mL | 11.0251 mL | 22.0502 mL | |
| 5 mM | 0.4410 mL | 2.2050 mL | 4.4100 mL | |
| 10 mM | 0.2205 mL | 1.1025 mL | 2.2050 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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