Chemical Structure : STK17A/B inhibitor 9
CAS No.:
3002038-21-0
STK17A/B inhibitor 9
Catalog No.: PC-22555Not For Human Use, Lab Use Only.
STK17A/B inhibitor 9 is a potent and selective, orally active STK17A/B inhibitor with IC50 of 23 nM (STK17A/DRAK1).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
STK17A/B inhibitor 9 is a potent and selective, orally active STK17A/B inhibitor with IC50 of 23 nM (STK17A/DRAK1).
STK17A/B inhibitor 9 shows high potency against STK17B (DRAK2) with 98.5% inhibition at 1 uM concentration.
STK17A/B inhibitor 9 shows moderate off-target inhibition only for AAK1, MYLK4, and NEK3/5, very low inhibitory potency against CLK4 (IC50 > 10,000 nM).
STK17A/B inhibitor 9 (1-10 uM) dose-dependently decreases STK17A, decreases levels of phosphorylated-p53 Serine-20 and phosphorylated-ILK Serine-246 on HEK293 cells overexpressing STK17A.
STK17A/B inhibitor 9 has EC50 values around or below 1 μM in several AML cell lines.
STK17A/B inhibitor 9 shows good oral bioavailability for in vivo efficacy studies in several AML PDX mouse models.
Physicochemical Properties
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M.Wt
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453.55
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Formula
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C26H27N7O
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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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N-isopropyl-4-((4-(2-(pyrrolidin-1-yl)quinazolin-6-yl)pyrimidin-2-yl)amino)benzamide
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References
1. Sana Chaudhry, et al. ACS Med Chem Lett. 2024 May 20;15(6):945-949.
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