| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
KAT6-IN-1 targets KAT6A and KAT6B (also known as MOZ and MORF, respectively), which are histone lysine acetyltransferases that catalyze the acetylation of histone H3 at lysine 23 (H3K23). These enzymes are involved in transcriptional regulation and have been implicated in various cancers. By inhibiting KAT6A and KAT6B, the compound disrupts histone acetylation, leading to altered gene expression and antitumor effects.
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| ln Vitro |
KAT6-IN-1 demonstrates potent in vitro inhibition of KAT6A and KAT6B histone acetyltransferase activity. It is a selective and orally available inhibitor with antitumor activity. The compound's activity is typically assessed in biochemical assays measuring histone acetylation, as well as in cell-based assays evaluating cancer cell proliferation and survival.
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| ln Vivo |
In vivo activity of KAT6-IN-1 is suggested by its oral availability and antitumor properties. The compound has potential for in vivo efficacy in animal models of cancer, particularly in tumors driven by KAT6A or KAT6B dysregulation. Further in vivo studies are needed to evaluate its pharmacokinetic properties, antitumor efficacy, and safety profile in appropriate animal models.
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| Enzyme Assay |
In vitro enzyme assays for KAT6-IN-1 involve measuring its inhibition of KAT6A and KAT6B histone acetyltransferase activity. The assay typically uses purified recombinant enzymes and histone substrates, with acetyltransferase activity measured by detecting acetylation using radioactive or fluorescence-based methods. IC50 values can be determined from dose-response curves generated in these enzymatic assays.
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| Cell Assay |
In vitro cellular assays for KAT6-IN-1 involve treating cancer cell lines with varying concentrations of the compound and measuring cell proliferation using MTT or other viability assays. Inhibition of KAT6 activity is assessed by measuring histone H3K23 acetylation levels using Western blotting or ELISA. The compound's antitumor activity is evaluated by assessing its effects on cancer cell growth and survival.
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| Animal Protocol |
In vivo animal experiments for KAT6-IN-1 would typically involve administering the compound orally to tumor-bearing mouse models. Efficacy is evaluated by measuring tumor growth inhibition, survival rates, and biomarker changes such as histone acetylation levels. The compound's oral bioavailability makes it suitable for oral dosing studies in cancer models.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for KAT6-IN-1 indicate that it is orally available, suggesting favorable absorption and bioavailability. The compound has a molecular weight of 414.44 and is soluble in DMSO at 4 mg/mL with ultrasonic and warming. Powder should be stored at -20°C for up to 3 years and at 4°C for up to 2 years. Its full ADME profile is being characterized.
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| Toxicity/Toxicokinetics |
Toxicological data for KAT6-IN-1 are limited. As a research compound, comprehensive toxicological studies have not been reported. The compound is intended for research use only and is not for human therapeutic application. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
KAT6-IN-1 (CAS#: 2569008-99-5) has the molecular formula C19H18N4O5S and a molecular weight of 414.44. It is also known as Prifetrastat and PF-07248144. The compound is a selective, orally available inhibitor of KAT6A and KAT6B with antitumor activity. Purity is ≥98%. It is for research use only.
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| Molecular Formula |
C19H18N4O5S
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|---|---|
| Molecular Weight |
414.435022830963
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| Exact Mass |
414.099
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| CAS # |
2569008-99-5
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| PubChem CID |
155411211
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| Appearance |
White to off-white solid powder
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| LogP |
2.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
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| Complexity |
645
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RCBWSTJGOASLEO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H18N4O5S/c1-26-14-6-3-4-7-17(14)29(24,25)22-19-18-15(27-2)10-13(11-16(18)28-21-19)12-23-9-5-8-20-23/h3-11H,12H2,1-2H3,(H,21,22)
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| Chemical Name |
2-methoxy-N-[4-methoxy-6-(pyrazol-1-ylmethyl)-1,2-benzoxazol-3-yl]benzenesulfonamide
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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)
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| Solubility (In Vitro) |
DMSO : 4 mg/mL (9.65 mM)
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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 | 2.4129 mL | 12.0645 mL | 24.1289 mL | |
| 5 mM | 0.4826 mL | 2.4129 mL | 4.8258 mL | |
| 10 mM | 0.2413 mL | 1.2064 mL | 2.4129 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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