PQR530

PQR530
  • Name: PQR530
  • Catalog No.: CPDB1536
  • CAS No.: 1927857-61-1
  • Molecular Weight: 407.4258
  • Chemical Formula: C18H23F2N7O2
  • For scientific research only, not for patients.

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    100mg In Stock 500
    500mg In Stock 800
    1g In Stock 1200
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    Chemical Name:

    (S)-4-(difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine

    SMILES Code: 

    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

    Keyword:

    PQR530, PQR-530, PQR 530, 1927857-61-1

    Solubility: Soluble in DMSO

    Storage: 0 - 4°C for short term (days to weeks), or -20°C for long term (months).

    Description: 

    PQR530 is a highly potent dual pan-PI3K/mTORC1/2 inhibitor. PQR530 inhibited protein kinase B (PKB, pSer473) and ribosomal protein S6 (pS6, pSer235/236) phosphorylation with IC50 values of 0.07 µM. PQR530 showed excellent selectivity over a wide panel of kinases, as well as excellent selectivity versus unrelated receptor enzymes and ion channels. Moreover, PQR530 displayed potency in a panel of 44 cancer cell lines (NTRC OncolinesTM) to prevent cancer cell growth (mean value for GI50 of 426 nM). Oral application of PQR530 to mice resulted in a dose-proportional PK and demonstrated good oral bioavailability and excellent brain penetration.

    Target: PI3K/mTOR


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