Chemical Structure : BEN-28010
CAS No.:
3033961-38-2
BEN-28010
(BEN28010)
Catalog No.: PC-24518Not For Human Use, Lab Use Only.
BEN-28010 is a potent selective, orally bioavailable and brain-penetrant checkpoint kinase 1 (CHK1) inhibitor with IC50 of 4 nM, 450-fold selective over CHK2.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
BEN-28010 is a potent selective, orally bioavailable and brain-penetrant checkpoint kinase 1 (CHK1) inhibitor with IC50 of 4 nM, 450-fold selective over CHK2.
BEN-28010 potently inhibits pCHK1 in SW620 cells with IC50 of 0.45 uM, inhibits LN-18/A172 cell viability with IC50 of 0.14/3.3 uM.
BEN-28010 also has good selectivity for CHK1 over the diverse Cerep SafetyScreen87 panel of 87 enzymes.
BEN-28010 demonstrated efficacy in several GBM CDX and PDX models as a monotherapy and in combination with ionizing radiation, including improved overall survival in an intracranially implanted GBM PDX mouse model.
Physicochemical Properties
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M.Wt
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374.45
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Formula
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C20H22N8
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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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(R)-5-((1-(4-(3-(Dimethylamino)pyrrolidin-1-yl)phenyl)-1H-imidazol-4-yl) amino)pyrazine-2-carbonitrile
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References
1. Rawling MJ, et al. J Med Chem. 2025 Apr 24. doi: 10.1021/acs.jmedchem.5c00279.
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