A dual inhibitor of PI3Kα and mTOR
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PQR530

Item No. 28563

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(difluoromethyl)-5-[4-[(3S)-3-methyl-4-morpholinyl]-6-(4-morpholinyl)-1,3,5-triazin-2-yl]-2-pyridinamine
CAS Number
1927857-61-1
Molecular Formula
C18H23F2N7O2
Formula Weight
407.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:3): 0.33 mg/mlDMSO: 10 mg/ml
λmax
235, 290 nm
SMILES
NC1=NC=C(C2=NC(N3[C@@H](C)COCC3)=NC(N4CCOCC4)=N2)C(C(F)F)=C1
InChi Code
InChI=1S/C18H23F2N7O2/c1-11-10-29-7-4-27(11)18-24-16(13-9-22-14(21)8-12(13)15(19)20)23-17(25-18)26-2-5-28-6-3-26/h8-9,11,15H,2-7,10H2,1H3,(H2,21,22)/t11-/m0/s1
InChi Key
SYKBZXMKAPICSO-NSHDSACASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $95

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    5 mg

    $256

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    10 mg

    $464

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    25 mg

    $1,037

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    Product Description

    PQR530 is a dual inhibitor of PI3Kα and mammalian target of rapamycin (mTOR; IC50s = 11.1 and 7.4 nM, respectively).1 It inhibits phosphorylation of Akt and ribosomal S6 kinase in A2058 melanoma cells (IC50s = 62.2 and 61.1 nM, respectively). PQR530 inhibits cell growth in a panel of 66 cancer cell lines (mean GI50 = 0.43 µM). In vivo, PQR530 (25 mg/kg) reduces tumor growth in an OVCAR-3 ovarian cancer mouse xenograft model. It decreases the number of seizures per week in a Tsc1GFAP conditional knockout mouse model of epilepsy.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rageot, D., Bohnacker, T., Keles, E., et al. (S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530, a potent, orally bioavailable and brain penetrable dual inhibitor of class I PI3K and mTOR kinase. J. Med. Chem. 62(13), 6241-6261 (2019).

    2. Theilmann, W., Gericke, B., Schidlitzki, A., et al. Novel brain permeant mTORC1/2 inhibitors are as efficacious as rapamycin or everolimus in mouse models of acquired partial epilepsy and tuberous sclerosis complex. Neuropharmacology 180, 108297 (2020).