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
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