Art. -Nr.: HY-168035

W4275

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W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC₅₀ value of 17 nM. W4275 exhibits antiproliferative activity with an IC₅₀ of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research.

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Reinheit: 98.93%
CAS. Nr.: 3051650-00-8
Formel: C₂₅H₃₆N₆O₃
Molecular Weight:468.59

Speicherung:

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

W4275 Chemical Structure

CAS. Nr.: 3051650-00-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

NSD2

17 nM (IC₅₀)

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
KMS-11	IC₅₀	17 μM Compound: 42	Antiproliferative activity against human KMS-11 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay Antiproliferative activity against human KMS-11 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay	[PMID: 39230932]
MOLM-13	IC₅₀	1.199 μM Compound: 42	Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay	[PMID: 39230932]
MOLT-4	IC₅₀	1.752 μM Compound: 42	Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay	[PMID: 39230932]
MV4-11	IC₅₀	1.384 μM Compound: 42	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay	[PMID: 39230932]
RS4-11	IC₅₀	0.23 μM Compound: 42	Antiproliferative activity against human RS4-11 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay Antiproliferative activity against human RS4-11 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay	[PMID: 39230932]

Chemical Information

CAS. Nr. 3051650-00-8
Appearance Solid
Molecular Weight 468.59
Formel C₂₅H₃₆N₆O₃
Color White to off-white
SMILES

CC(N1CCC(NC2=NC(C#N)=NC3=CC(OCCCN4CCOCC4)=C(C=C32)OC)CC1)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (266.76 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

2.1341 mL

10.6703 mL

21.3406 mL

5 mM

0.4268 mL

2.1341 mL

4.2681 mL

10 mM

0.2134 mL

1.0670 mL

2.1341 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: ≥ 6.25 mg/mL (13.34 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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% Corn Oil

Solubility: ≥ 6.25 mg/mL (13.34 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 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 (62.5 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 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]. Wei J, et al. Discovery of a Highly Potent and Selective Inhibitor Targeting Protein Lysine Methyltransferase NSD2. J Med Chem. 2024 Sep 4. [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	2.1341 mL	10.6703 mL	21.3406 mL	53.3515 mL
	5 mM	0.4268 mL	2.1341 mL	4.2681 mL	10.6703 mL
	10 mM	0.2134 mL	1.0670 mL	2.1341 mL	5.3352 mL
	15 mM	0.1423 mL	0.7114 mL	1.4227 mL	3.5568 mL
	20 mM	0.1067 mL	0.5335 mL	1.0670 mL	2.6676 mL
	25 mM	0.0854 mL	0.4268 mL	0.8536 mL	2.1341 mL
	30 mM	0.0711 mL	0.3557 mL	0.7114 mL	1.7784 mL
	40 mM	0.0534 mL	0.2668 mL	0.5335 mL	1.3338 mL
	50 mM	0.0427 mL	0.2134 mL	0.4268 mL	1.0670 mL
	60 mM	0.0356 mL	0.1778 mL	0.3557 mL	0.8892 mL
	80 mM	0.0267 mL	0.1334 mL	0.2668 mL	0.6669 mL
	100 mM	0.0213 mL	0.1067 mL	0.2134 mL	0.5335 mL

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W4275

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

W4275

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

W4275 Related Classifications

HY-168035 Related Classifications