Mosipasertib (ATRN-119) | ATR inhibitor

Chemical Structure : Mosipasertib

Mosipasertib (ATRN-119, ATRN 119, ATRN119)

Catalog No.: PC-27479Not For Human Use, Lab Use Only.

Mosipasertib (ATRN-119) is a potent, highly selective orally bioavailable macrocyclic ATR inhibitor with IC50 of approximately 4 nM.

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Biological Activity

Mosipasertib (ATRN-119) is a potent, highly selective orally bioavailable macrocyclic ATR inhibitor with IC50 of approximately 4 nM.
ATRN-119 exhibits significant selectivity over other key PIKK family members, including ATM, DNA-PK, and mTOR, with IC50 values that are over 600-fold, 2000-fold, and 2000-fold higher, respectively.
ATRN-119 effectively limits the viability of various cancer cell lines, with EC50 values in the low nanomolar range.
ATRN-119 demonstrates a dose-dependent decrease in the phosphorylation of Checkpoint Kinase 1 (CHK1) on Serine 345, a direct downstream target of ATR, also increases the phosphorylation of H2AX, a marker of DNA double-strand breaks, indicating the collapse of replication forks.
ATRN-119 is being studied in advanced solid tumors with dysregulated components of the DNA damage response (DDR).

Physicochemical Properties

M.Wt	556.64
Formula	C26H32N6O6S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	12,15-Etheno-16,20-nitrilo-8H,20H-1,4,7,11,10,18,22-benzotrioxathiatriazacyclotetracosin-21(22H)-one, 19-amino-2,3,5,6,9,10-hexahydro-10-methyl-26-[(methylamino)methyl]-, 11,11-dioxide

References

1. Patent US20160102104 A1 2016-04-14.

2. Patnet WO2016061097 A1 2016-04-21.

Mosipasertib (ATRN-119, ATRN 119, ATRN119)

Biological Activity

Physicochemical Properties

References

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