A MAT2A inhibitor
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AG-270

Item No. 36246

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(1-cyclohexen-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridinylamino)-pyrazolo[1,5-a]pyrimidin-7(4H)-one
CAS Number
2201056-66-6
Molecular Formula
C30H27N5O2
Formula Weight
489.6
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble
λmax
273, 317 nm
SMILES
O=C1C(C2=CC=C(OC)C=C2)=C(NC3=C(C4=CCCCC4)C(C5=CC=CC=C5)=NN13)NC6=CC=CC=N6
InChi Code
InChI=1S/C30H27N5O2/c1-37-23-17-15-21(16-18-23)26-28(32-24-14-8-9-19-31-24)33-29-25(20-10-4-2-5-11-20)27(34-35(29)30(26)36)22-12-6-3-7-13-22/h3,6-10,12-19,33H,2,4-5,11H2,1H3,(H,31,32)
InChi Key
HSVRUECLQUGTDS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $246

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    10 mg

    $466

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    25 mg

    $919

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    50 mg

    $1,468

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    Cayman Chemical
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    Product Description

    AG-270 is an inhibitor of methionine adenosyltransferase 2A (MAT2A; IC50 = 0.014 µM).1 It reduces levels of S-(5'-adenosyl)-L-methonine (SAM; Item Nos. 16376 | 17595) in, and inhibits the proliferation of, HCT116 cells with a homozygous deletion of MTAP, the gene encoding methylthioadenosine phosphorylase (IC50s = 0.2 and 0.257 µM, respectively). AG-270 (200 mg/kg) reduces intratumor SAM levels and tumor growth in KP4 and HCT116 MTAP-null, but not HCT116 MTAP-wild-type, mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Konteatis, Z., Travins, J.G., S., Marjon, K., et al. Discovery of AG-270, a first-in-class oral MAT2A inhibitor for the treatment of tumors with homozygous MTAP deletion. J. Med. Chem. 64(8), 4430-4449 (2021).