M3814 (Nedisertib, Peposertib) | DNA-PK inhibitor

Chemical Structure : M3814

CAS No.: 1637542-33-6

M3814 (Peposertib; Nedisertib; M 3814; MSC2490484A)

Catalog No.: PC-61389Not For Human Use, Lab Use Only.

M3814 (Nedisertib, Peposertib, MSC2490484A) is a highly potent, selective, ATP-competitive and orally bioavailable inhibitor of DNA-PK with IC50 of 0.6 nM (10 uM ATP).

Packing	Price	Stock
5 mg	$148	In stock
10 mg	$228	In stock
25 mg	$398	In stock
50 mg	$598	In stock
100 mg		Get quote

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Biological Activity

M3814 (Nedisertib, Peposertib, MSC2490484A) is a highly potent, selective, ATP-competitive and orally bioavailable inhibitor of DNA-PK with IC50 of 0.6 nM (10 uM ATP).

M3814 exhibited a high degree of selectivity when tested using a broad panel of serine/threonine, tyrosine, and lipid kinases, only 8of 284 recombinantly expressed protein/lipid kinases, including mutant kinases, were inhibited by at least 50% at 1 μmol/L M3814.

M3814 selectively inhibits DNA-PK activity and DSB repair in human cancer cell lines.

M3814 sensitizes cancer cells to IR through impaired colony outgrowth or proliferation/viability.

M3814 inhibits radiation-induced DNA-PK autophosphorylation and DSB repair in tumor xenograft models.

M3814 in combination with ionizing radiation (IR) has antitumor activity in mouse xenograft models.

Physicochemical Properties

M.Wt	481.912
Formula	C24H21ClFN5O3
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	(S)-{2-chloro-4-fluoro-5-[7-(morpholin-4-yl)quinazolin-4-yl]phenyl}(6-methoxypyridazin-3-yl)methanol

References

1. Harnor SJ, et al. ChemMedChem. 2017 Jun 21;12(12):895-900.
2. Zenke FT, et al. Mol Cancer Ther. 2020 May;19(5):1091-1101.

M3814 (Peposertib; Nedisertib; M 3814; MSC2490484A)

Biological Activity

Physicochemical Properties

References

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