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PQR620

CAS No. : 1927857-56-4

MCE 站：PQR620

产品活性：PQR620 是一种有效的，具有口服活性的可透过血脑屏障的选择性 mTORC1/2 抑制剂。

研究领域：PI3K/Akt/mTOR

作用靶点：mTOR

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

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).

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