Art. -Nr.: HY-152241

DS-9300

Name: DS-9300
Brand: MedChemExpress
SKU: HY-152241
Price: 325.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC₅₀ value of 28 nM. DS-9300 has anticancer activity and can be used in prostate cancer disease research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.83%
CAS. Nr.: 2259641-46-6
Formel: C₂₅H₂₆F₃N₅O₃
Molecular Weight:501.50

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

DS-9300 Chemical Structure

CAS. Nr.: 2259641-46-6

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (1)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC₅₀ value of 28 nM. DS-9300 has anticancer activity and can be used in prostate cancer disease research^[1].

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	GI₅₀	6.5 nM Compound: 16; DS-9300	Antiproliferative activity against AR-positive human 22Rv1 cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay Antiproliferative activity against AR-positive human 22Rv1 cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay	[PMID: 36572866]
LNCaP	GI₅₀	3.4 nM Compound: 16; DS-9300	Antiproliferative activity against AR-positive human LNCaP cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay Antiproliferative activity against AR-positive human LNCaP cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay	[PMID: 36572866]
PC-3	GI₅₀	287.2 nM Compound: 16; DS-9300	Antiproliferative activity against AR-negative human PC-3 cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay Antiproliferative activity against AR-negative human PC-3 cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay	[PMID: 36572866]
VCaP	GI₅₀	0.6 nM Compound: 16; DS-9300	Antiproliferative activity against AR-positive human VCaP cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay Antiproliferative activity against AR-positive human VCaP cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay	[PMID: 36572866]

In Vitro

DS-9300 inhibits the growth of prostate cancer cell lines with the IC₅₀ values of 0.6, 6.5, 3.4 and 287.2 nM for VCaP, 22Rv1, LNCaP and PC3 cells, respectively, indicating that it could effectively inhibit the growth of prostate cancer cell lines by inhibiting histone acetylation and down-regulating PSA expression^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

In Vivo

DS-9300 (p.o., 0.3-3 mg/kg, once daily, 33days) shows dose-dependent antitumor activity with 39%, 74% and 109% tumor growth inhibition at 0.3, 1 and 3 mg/kg, respectively, and no significant toxic effects in Castrated VCaP xenograft mouse model^[1].
The pharmacokinetic parameters of DS-9300 in BALB/c mice

PO(10 mg/kg)			IV(1 mg/kg)
AUC, AUC_u (μM*h)	C_max (μM)	T_1/2 (h)<	Vd_ss (L/kg)	CL, CL_u (mL/min/kg)	F%
130, 5.33	34	2.4	0.14	1.6, 39	62

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

Chemical Information

CAS. Nr. 2259641-46-6
Appearance Solid
Molecular Weight 501.50
Formel C₂₅H₂₆F₃N₅O₃
Color White to off-white
SMILES

COC1=CC=C(C=C1)C2(CCC(F)(CC2)F)C(N3C[C@@H](C[C@@H]3C(NC4=NC5=C(NN=C5)C=C4)=O)F)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (199.40 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

1.9940 mL

9.9701 mL

19.9402 mL

5 mM

0.3988 mL

1.9940 mL

3.9880 mL

10 mM

0.1994 mL

0.9970 mL

1.9940 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 5 mg/mL (9.97 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (9.97 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (9.97 mM); Clear solution

This protocol yields a clear solution of ≥ 5 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 (50.0 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

Protokoll

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Handling Instructions (2659 KB)

Verweise

[1]. Ryutaro Kanada, et al. Discovery of DS-9300: A Highly Potent, Selective, and Once-Daily Oral EP300/CBP Histone Acetyltransferase Inhibitor. J Med Chem. 2023 Jan 12;66(1):695-715. [Content Brief]

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, 6 months; -20°C, 1 month. 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	1 mM	1.9940 mL	9.9701 mL	19.9402 mL	49.8504 mL
	5 mM	0.3988 mL	1.9940 mL	3.9880 mL	9.9701 mL
	10 mM	0.1994 mL	0.9970 mL	1.9940 mL	4.9850 mL
	15 mM	0.1329 mL	0.6647 mL	1.3293 mL	3.3234 mL
	20 mM	0.0997 mL	0.4985 mL	0.9970 mL	2.4925 mL
	25 mM	0.0798 mL	0.3988 mL	0.7976 mL	1.9940 mL
	30 mM	0.0665 mL	0.3323 mL	0.6647 mL	1.6617 mL
	40 mM	0.0499 mL	0.2493 mL	0.4985 mL	1.2463 mL
	50 mM	0.0399 mL	0.1994 mL	0.3988 mL	0.9970 mL
	60 mM	0.0332 mL	0.1662 mL	0.3323 mL	0.8308 mL
	80 mM	0.0249 mL	0.1246 mL	0.2493 mL	0.6231 mL
	100 mM	0.0199 mL	0.0997 mL	0.1994 mL	0.4985 mL

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DS-9300

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen