Chemical Structure : G9a/NSD2 dual inhibitor 16
CAS No.:
2761292-51-5
G9a/NSD2 dual inhibitor 16
(W4032)
Catalog No.: PC-22701Not For Human Use, Lab Use Only.
G9a/NSD2 dual inhibitor 16 (W4032) is a highly potent G9a/NSD2 dual inhibitor with IC50 of 241/17 nM respectively, shows potent cell growth inhibition against PANC-1 and MDA-MB-231 with IC50 values of 0.44 and 0.72 μM, respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
G9a/NSD2 dual inhibitor 16 (W4032) is a highly potent G9a/NSD2 dual inhibitor with IC50 of 241/17 nM respectively, shows potent cell growth inhibition against PANC-1 and MDA-MB-231 with IC50 values of 0.44 and 0.72 μM, respectively.
G9a/NSD2 dual inhibitor 16 has an IC50 of 0.41 μM for the GLP, shows selectivity over PRMT1 (IC60=6.44 uM) and has no activity for PRMT4, PRMT5, EZH2, MLL1, MLL4 and DNMT1 up to 10 μM.
G9a/NSD2 dual inhibitor 16 significantly inhibis the colony formation of MDA-MB-231 and PANC-1 cells in a dose-dependent manner, induces apoptosis.
G9a/NSD2 dual inhibitor 16 inhibits invasion of MDA-MB-231 and PANC-1 cells dose-dependently.
G9a/NSD2 dual inhibitor 16 (4-16 mg/kg) exhibits vivo antitumor activity in PANC-1 cell-derived xenograft.
Physicochemical Properties
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M.Wt
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452.60
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Formula
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C25H36N6O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4-[(1-Isopropylpiperidin-4-yl)amino]-6-methoxy-7-[3-(pyrrolidin-1-yl)propoxy]quinazoline-2-carbonitrile
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References
1. Chunju Yang, et al. J Med Chem. 2024 Jul 15. doi: 10.1021/acs.jmedchem.4c00640.
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