PQR-620

CAS No. 1927857-56-4

PQR-620( PQR620 )

Catalog No. M13021 CAS No. 1927857-56-4

PQR-620 (PQR620) is a novel potent and selective, brain penetrant inhibitor of mTORC1/2.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 230 Get Quote
10MG 332 Get Quote
25MG 560 Get Quote
50MG 797 Get Quote
100MG 1071 Get Quote
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Biological Information

  • Product Name
    PQR-620
  • Note
    Research use only, not for human use.
  • Brief Description
    PQR-620 (PQR620) is a novel potent and selective, brain penetrant inhibitor of mTORC1/2.
  • Description
    PQR-620 (PQR620) is a novel potent and selective, brain penetrant inhibitor of mTORC1/2; displays >1000-fold selectivity towards mTOR over PI3Kα in enzymatic binding assays; demonstrates inhibition of protein kinase B (pSer473) and ribosomal protein S6 (pSer235/236) phosphorylation with IC50 of 0.2 uM and 0.1 uM, respectively; shows anti-tumor effects in vitro and in vivo.
  • In Vitro
    PQR620 is a potent and selective mTOR inhibitor, which induces >1000-fold selectivity towards mTOR over PI3Kα in enzymatic binding assays. In A2058 melanoma cells PQR620 demonstrates inhibition of protein kinase B (pSer473) and ribosomal protein S6 (pSer235/236) phosphorylation with IC50 values of 0.2 μM and 0.1 μM, respectively. PQR620 shows excellent selectivity over a wide panel of kinases, as well as excellent selectivity versus unrelated receptor enzymes and ion channels. PQR620 demonstrates its potency to prevent cancer cell growth in an NTRC 44 cancer cell line panel, resulting in a 10log(IC50) of 2.86 (nM). PQR620 has a median IC50 of 250 nM when tested on 44 lymphoma cell lines. Activity is higher in B cell than in T cell tumors (median IC50s: 250 nM vs 450 nM; P=0.002). At 72h, anti-tumor activityof PQR620 is mostly cytostatic and apoptosis induction is seen only in 6/44 cell lines (13%). Sensitivity to PQR620 or apoptosis induction does not differ between DLBCL and MCL, and they are not affected by the DLBCL cell of origin, by TP53 status or by the presence of MYC or BCL2 translocations.
  • In Vivo
    The physico-chemical properties of PQR620 result in good oral bioavailability and excellent brain penetration. The activity of PQR620 as single agent undergoes in vivo evaluation in two DLBCL models, the germinal center B cell type DLBCL (GCB-DLBCL) SU-DHL-6 and the acivated B cell-like DLBCL (ABC-DLBCL) RIVA. Treatments with PQR620 (100 mg/kg dose per day, Qd×7/w) start with 100-150 mm3 tumors and are carried for 14 (SU-DHL-6) or 21 days (RIVA). In both models, PQR620 determines a 2-fold decrease of the tumor volumes in comparison with control, with significant differences in both SU-DHL-6 (D7, D9, D11, D14; P<0.005) and RIVA (D14, D16, D19, D21; P<0.005).
  • Synonyms
    PQR620
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    mTOR
  • Recptor
    mTOR
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    1927857-56-4
  • Formula Weight
    445.4657
  • Molecular Formula
    C21H25F2N7O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 6.4 mg/mL (Need warming)
  • SMILES
    NC1=NC=C(C2=NC(N3C4COCC3CC4)=NC(N5C6COCC5CC6)=N2)C(C(F)F)=C1
  • Chemical Name
    5-(4,6-di((1R,5S)-3-oxa-8-azabicyclo[3.2.1]octan-8-yl)-1,3,5-triazin-2-yl)-4-(difluoromethyl)pyridin-2-amine

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Florent Beaufils, et al. Cancer Res, Abstract 1336 DOI: 10.1158/1538-7445.AM2016-1336 Published July 2016
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