Referencia número: HY-132283

PF-9363

(Synonyms: CTx-648)

5 Cited Publications

Revisión del cliente

Based on 5 publication(s) in Google Scholar

PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.64%
No. CAS: 2569009-58-9
Fòrmula: C₂₀H₂₀N₄O₆S
Peso molecular:444.46

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

PF-9363 Chemical Structure

No. CAS: 2569009-58-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer^[1]^[2].

IC₅₀ & Target

MOZ/MORF

Ver todos los productos específicos de isoformas Histone Acetyltransferase :

In Vitro

PF-9363 (0~1 μM; 1 day; ZR75-1, T47D and MCF7 cells) down-regulates the expression of H3K23Ac biomarker^[1].
PF-9363 leads to down regulation of a specific set of genes involved in ESR1 pathway, cell cycle and stem cell pathways. PF-9363 shows that the IC₅₀ values for ZR75-1 and T47D are 0.3 nM and 0.9 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

ZR75-1, T47D and MCF7 cells
Concentration:

0~1 μM
Incubation Time:

1 day
Result:

Down-regulated the expression of H3K23Ac biomarker.

In Vivo

PF-9363 shows strong anti-tumor activity in patient-derived xenograft models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

No. CAS 2569009-58-9
Appearance Solid
Peso molecular 444.46
Fòrmula C₂₀H₂₀N₄O₆S
Color White to off-white
SMILES

O=S(C1=C(OC)C=CC=C1OC)(NC2=NOC3=C2C(OC)=CC(CN4N=CC=C4)=C3)=O
Synonyms

CTx-648
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (5)

All WBFlow CytometryCell Proliferation/Viability AssayBio/Physico-chemical Assay

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Journal Impact Factor

Nat Cell Biol

KDM6A epigenetically regulates subtype plasticity in small cell lung cancer. [Abstract]

2023 Sep;25(9):1346-1358. PMID: 37591951

PF-9363 purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2023 Sep;25(9):1346-1358. [Abstract]

Immunoblot analysis of 1014 Kdm6a isogenic cells treated with inhibitors that block the function of epigenetic modifiers that normally maintain gene expression including VTP50469 (500 nM), EPZ-5676 (1 μM), PF-9363 (100 nM), JQAD1 or DMSO for 6 days.
Blood Cancer Discov

2026 Apr 19.
Am J Physiol Cell Physiol

The role of KAT6A in regulating primordial follicle activation in mouse ovary. [Abstract]

2025 Jul 1;329(1):C38-C49. PMID: 40434042
bioRxiv

MYST acetyltransferases are a targetable therapeutic vulnerability in SETBP1-mutant leukemia. [Abstract]

2026 Jan 8:2026.01.08.697228. PMID: 41542431
bioRxiv

KAT6A/B inhibition synergizes with retinoic acid and enhances the efficacy of GD2-targeted immunotherapy in neuroblastoma. [Abstract]

2025 Jul 2:2025.07.01.662644. PMID: 40631259

PF-9363 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 2:2025.07.01.662644. [Abstract]

Western blot analysis using antibodies to the indicated histones that were extracted from neuroblastoma cell line KELLY after treatment with the indicated doses of PF-9363 (0-10 μM) for 1, 3 and 6 days. Total H3 served as a loading control.

PF-9363 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 2:2025.07.01.662644. [Abstract]

Flow cytometry showing GD2 expression levels in the GD2low cell lines BE2C, NGP and NB1 treated for 14 days with DMSO, isotretinoin alone, PF9363 (1 μM) alone, or isotretinoin plus PF-9363.

PF-9363 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 2:2025.07.01.662644. [Abstract]

Cell viability of BE2C and NB1 cells following both treatment with either DMSO, isotretinoin alone, PF-9363 alone, or isotretinoin plus PF-9363 (1 μM) for 14 days and subsequent, co-culture with NK cells and dinutuximab for 24 hours.

PF-9363 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 2:2025.07.01.662644. [Abstract]

Scatter plot of log2 fold-changes in H3K27me3 CUT&RUN signal at significant islands with lfc > 0.5 versus their fold-change rank. Experiments obtained from BE2C cells treated with PF-9363, isotretinoin or isotretinoin plus PF-9363 for 14 days at a concentration of 1 μM compared to control DMSO-treated BE2C cells. Significant islands associated with PHOX2B and GATA3 are noted.

PF-9363 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 2:2025.07.01.662644. [Abstract]

Western-blot assay for transcription factors GATA3, PHOX2B and MYCN in BE2C cells treated with isotretinoin plus PF-9363 (1 μM) for 14 days followed by PF-9363 alone for 28 days.

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (112.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (4.68 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (4.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Shikhar S, et al. First-in-class KAT6A/KAT6B Inhibitor CTx-648 (PF-9363) Demonstrates Potent Anti-tumor Activity in ER+ Breast Cancer with KAT6A Dysregulation

[2]. WO2020254946

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2499 mL	11.2496 mL	22.4992 mL	56.2480 mL
	5 mM	0.4500 mL	2.2499 mL	4.4998 mL	11.2496 mL
	10 mM	0.2250 mL	1.1250 mL	2.2499 mL	5.6248 mL
	15 mM	0.1500 mL	0.7500 mL	1.4999 mL	3.7499 mL
	20 mM	0.1125 mL	0.5625 mL	1.1250 mL	2.8124 mL
	25 mM	0.0900 mL	0.4500 mL	0.9000 mL	2.2499 mL
	30 mM	0.0750 mL	0.3750 mL	0.7500 mL	1.8749 mL
	40 mM	0.0562 mL	0.2812 mL	0.5625 mL	1.4062 mL
	50 mM	0.0450 mL	0.2250 mL	0.4500 mL	1.1250 mL
	60 mM	0.0375 mL	0.1875 mL	0.3750 mL	0.9375 mL
	80 mM	0.0281 mL	0.1406 mL	0.2812 mL	0.7031 mL
	100 mM	0.0225 mL	0.1125 mL	0.2250 mL	0.5625 mL

Keywords

PF-9363

5 Cited Publications

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PF-9363

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Epigenetics Compound Library Mini

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) PF-9363

Ver todos los productos específicos de isoformas Histone Acetyltransferase

Actividad biológica

Chemical Information

Publications (5)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

PF-9363

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Epigenetics Compound Library Mini

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) PF-9363

Ver todos los productos específicos de isoformas Histone Acetyltransferase

Actividad biológica

Chemical Information

Publications (5)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

PF-9363 Related Classifications

HY-132283 Related Classifications