| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
PF-9363 targets KAT6A (lysine acetyltransferase 6A, also known as MOZ) and KAT6B (also known as MORF). PF-9363 is a potent and selective KAT6A/6B inhibitor with Ki values of 0.41 nM for KAT6A and 1.2 nM for KAT6B. It is selective for KAT6A and KAT6B over KAT7, KAT5, and KAT8 (Kis = 70, 420, and 670 nM, respectively).
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| ln Vitro |
The H3K23Ac biomarker is down-regulated in ZR75-1, T47D, and MCF7 cells when exposed to PF-9363 (0~1 μM; 1 day) [1]. A subset of genes implicated in the ESR1 pathway, cell cycle, and stem cell pathways are downregulated by PF-9363. ZR75-1 and T47D had IC50 values of 0.3 nM and 0.9 nM in PF-9363[1].
In vitro, PF-9363 is a potent and selective KAT6A/6B inhibitor with Ki values of 0.41 nM for KAT6A and 1.2 nM for KAT6B. It displays potent anti-tumor activity in ER+ breast cancer models. The compound is a first-in-class inhibitor of KAT6A/6B. |
| ln Vivo |
PF-9363 revealed strong anticancer efficacy in patient-derived xenograft models [1].
In vivo activity data for PF-9363 are not extensively detailed in the available sources. The compound displays potent anti-tumor activity in ER+ breast cancer models. It can be used for the research of cancer. Specific in vivo efficacy data in animal models have not been reported. |
| Enzyme Assay |
The in vitro enzyme assay for PF-9363 involves measuring the inhibition of KAT6A and KAT6B acetyltransferase activity. Recombinant KAT6A or KAT6B is incubated with a histone substrate and acetyl-CoA in the presence of varying compound concentrations. The Ki values of 0.41 nM for KAT6A and 1.2 nM for KAT6B are determined from dose-response curves.
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| Cell Assay |
Western Blot analysis [1]
Cell Types: ZR75-1, T47D and MCF7 cells Tested Concentrations: 0~1 μM Incubation Duration: 1 day Experimental Results: The expression of H3K23Ac biomarker was down-regulated. Cellular assays for PF-9363 are performed using ER+ breast cancer cell lines or other cancer cell lines. Cells are treated with PF-9363 at various concentrations. Histone acetylation is assessed by Western blotting. Cell proliferation and viability are measured using standard assays. |
| Animal Protocol |
In vivo animal studies for PF-9363 are conducted in ER+ breast cancer models. Tumor-bearing mice are treated with PF-9363. Tumor growth inhibition is measured. The compound's anti-tumor activity is assessed.
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| ADME/Pharmacokinetics |
PF-9363 has a molecular weight of 444.46 g/mol and a molecular formula of C20H20N4O6S. It is soluble in DMSO at 89 mg/mL (200.24 mM). Specific PK parameters such as half-life, bioavailability, and clearance have not been reported.
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| Toxicity/Toxicokinetics |
Toxicity data for PF-9363 are not reported in the available sources. As a research compound, it is not intended for therapeutic use. The compound has been evaluated in preclinical models, but specific toxicological profiles have not been characterized.
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| References | |
| Additional Infomation |
PF-9363 is a research compound for studying KAT6A/6B function in cancer epigenetics. It is a first-in-class, potent, and selective KAT6A/6B inhibitor with Ki values of 0.41 nM for KAT6A and 1.2 nM for KAT6B. The compound displays potent anti-tumor activity in ER+ breast cancer models. It is available from commercial suppliers for research use only.
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| Molecular Formula |
C20H20N4O6S
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|---|---|
| Molecular Weight |
444.461003303528
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| Exact Mass |
444.11
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| CAS # |
2569009-58-9
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| PubChem CID |
155411202
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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 |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
31
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| Complexity |
680
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C(=CC=CC=1OC)OC)(NC1C2C(=CC(CN3C=CC=N3)=CC=2ON=1)OC)(=O)=O
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| InChi Key |
VNSQFPFWUAZOTQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H20N4O6S/c1-27-14-6-4-7-15(28-2)19(14)31(25,26)23-20-18-16(29-3)10-13(11-17(18)30-22-20)12-24-9-5-8-21-24/h4-11H,12H2,1-3H3,(H,22,23)
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| Chemical Name |
2,6-dimethoxy-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 : ~50 mg/mL (~112.50 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (4.68 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2499 mL | 11.2496 mL | 22.4992 mL | |
| 5 mM | 0.4500 mL | 2.2499 mL | 4.4998 mL | |
| 10 mM | 0.2250 mL | 1.1250 mL | 2.2499 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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