W4275

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[1].

Product Specifications

CAS Number

[3051650-00-8]

UNSPSC

12352005

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/w4275.html

Purity

98.93

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C25H36N6O3

Molecular Weight

468.59

References & Citations

[1]Wei J, et al. Discovery of a Highly Potent and Selective Inhibitor Targeting Protein Lysine Methyltransferase NSD2. J Med Chem. 2024 Sep 4.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

NSD2/MMSET/WHSC1

Available Sizes

Curated Selection

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