AG-270 (C008B-266437)

AG-270 demonstrates potent reduction in levels of intracellular SAM , as well as MTAP-–selective antiproliferative activity in the HCT116 MTAP isogenic cell model in vitro. AG-270 exhibits an IC 50 of 20 nM in HCT116 MTAP- cell SAM at 72 h. MAT2A is a key enzyme in the methionine salvage pathway, responsible for generating the universal methyl donor, S-adenosylmethionine (SAM). In Vivo：AG-270 shows excellent microsomal, hepatocyte, and in vivo metabolic stability across species (human, mouse, rat, dog, and monkey). AG-270 exhibits T1/2 values of 5.9 h, 4.2 h, 4.8 h and 21.3 h in mouse, rat, monkey and dog, respectively . AG-270 (200 mg/kg, orally, q.d. for 38 days) results in dose-dependent reduction in tumor SAM levels and tumor growth of KP4 MTAP- xenografts and is well tolerated, with mean body weight loss <5% . Combining AG-270 with taxanes and gemcitabine yielded additive-tosynergistic antitumor activity, with the docetaxel combination yielding 50% complete tumor regressions in select models; combination benefits are observed in PDX models derived from esophageal, NSCLC, and pancreatic cancers.

Specifications & Purity: AG-270 demonstrates potent reduction in levels of intracellular SAM , as well as MTAP-–selective antiproliferative activity in the HCT116 MTAP isogenic cell model in vitro. AG-270 exhibits an IC 50 of 20 nM in HCT116 MTAP- cell SAM at 72 h. MAT2A is a key enzyme in the methionine salvage pathway, responsible for generating the universal methyl donor, S-adenosylmethionine (SAM). In Vivo：AG-270 shows excellent microsomal, hepatocyte, and in vivo metabolic stability across species (human, mouse, rat, dog, and monkey). AG-270 exhibits T1/2 values of 5.9 h, 4.2 h, 4.8 h and 21.3 h in mouse, rat, monkey and dog, respectively . AG-270 (200 mg/kg, orally, q.d. for 38 days) results in dose-dependent reduction in tumor SAM levels and tumor growth of KP4 MTAP- xenografts and is well tolerated, with mean body weight loss <5% . Combining AG-270 with taxanes and gemcitabine yielded additive-tosynergistic antitumor activity, with the docetaxel combination yielding 50% complete tumor regressions in select models; combination benefits are observed in PDX models derived from esophageal, NSCLC, and pancreatic cancers.

Grade: Moligand™

Molecular Formula: C30H27N5O2

Molecular Weight: 489.57

PubChem CID: 134307820

Isomeric SMILES: COC1=CC=C(C=C1)C2=C(N=C3C(=C(NN3C2=O)C4=CC=CC=C4)C5=CCCCC5)NC6=CC=CC=N6

Storage Temperature: Store at -20°C

Shipped in: Ice chest + Ice pads