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AG-270

Chemical Structure : AG-270

CAS No.: 2201056-66-6

AG-270 (AG270)

Catalog No.: PC-72638Not For Human Use, Lab Use Only.

AG-270 (AG270) is a highly potent, selective, orally bioavailable MAT2A inhibitor with IC50 of 14 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

AG-270 (AG270) is a highly potent, selective, orally bioavailable methionine adenosyltransferase 2A (MAT2A) inhibitor with IC50 of 14 nM.
AG-270 demonstrated potent reduction in levels of intracellular SAM, as well as MTAP-null-selective antiproliferative activity in the HCT116 MTAP isogenic cell model in vitro ((IC50=20 nM).
AG-270 (200 mg/kg q.d.) dose-dependently reduced tumor SAM levels and tumor growthpancreatic KP4 MTAP-null xenograft mouse model.
AG-270 showed excellent microsomal, hepatocyte, and in vivo metabolic stability across species (human, mouse, rat, dog, and monkey).

Physicochemical Properties

M.Wt 489.579
Formula C30H27N5O2
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

3-(cyclohex-1-en-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(pyridin-2-ylamino)pyrazolo[1,5-a]pyrimidin-7(4H)-one

References

1. Kalev P, et al. Cancer Cell. 2021 Feb 8;39(2):209-224.e11.

2. Konteatis Z, et al. J Med Chem. 2021 Apr 22;64(8):4430-4449.

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