Chemical Structure : BR101801
CAS No.:
2055765-77-8
BR101801
(BR-101801)
Catalog No.: PC-22675Not For Human Use, Lab Use Only.
BR101801 is a triple inhibitor of PI3Kγ/δ and DNA-PK, sensitizes radiation-induced DNA damage in various human solid cancer cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
BR101801 is a triple inhibitor of PI3Kγ/δ and DNA-PK, sensitizes radiation-induced DNA damage in various human solid cancer cells.
BR101801 inhibits not only the signal affecting cell growth caused by PI3Kγ/δ but also efficiently induces cell cycle arrest and apoptosis through inhibition of DNA-PK activation, with this triple target inhibition it decreases the stability of oncogenic protein, c-Myc.
BR101801 inhibited not only phosphorylation of DNA-PK catalytic subunit in NHEJ factors but also BRCA2 protein level in homologous recombination (HR) factors.
BR101801 enhances radiation response in various human solid cancer cell lines. BR101801 enhanced radiosensitivity in MDA-MB-231 xenografts via inhibition of phosphorylated DNA-PKcs.
BR101801 synergistically inhibited tumor growth in the HCT116 p53(-/-) xenograft mouse model.
Physicochemical Properties
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M.Wt
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478.33
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Formula
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C24H17Cl2N5O2
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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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(S)-4-((1-(4,8-dichloro-1-oxo-2-phenyl-1,2-dihydroisoquinolin-3-yl)ethyl)amino)pyrido[2,3-d]pyrimidin-5(1H)-one
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References
1. Seungho Wang, et al. Cancer Res (2020) 80 (16_Supplement): 4439.
2. Lee JH, et al. Am J Cancer Res. 2021 Nov 15;11(11):5440-5451.
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