1. PI3K/Akt/mTOR
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  3. PQR620

PQR620 

Cat. No.: HY-100026 Purity: 98.06%
Handling Instructions

PQR620 is a novel potent and selective brain penetrant inhibitor of mTORC1/2.

For research use only. We do not sell to patients.

PQR620 Chemical Structure

PQR620 Chemical Structure

CAS No. : 1927857-56-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 412 In-stock
Estimated Time of Arrival: December 31
1 mg USD 168 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
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Description

PQR620 is a novel potent and selective brain penetrant inhibitor of mTORC1/2.

IC50 & Target[1]

mTORC1

 

mTORC2

 

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)[1]. 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[2].

In Vivo

The physico-chemical properties of PQR620 result in good oral bioavailability and excellent brain penetration[1]. 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)[2].

Molecular Weight

445.47

Formula

C₂₁H₂₅F₂N₇O₂

CAS No.

1927857-56-4

SMILES

[H][[email protected]]1(CC[[email protected]]([H])2COC1)N2C3=NC(N4[[email protected]]5([H])CC[[email protected]]([H])4COC5)=NC(C6=CN=C(N)C=C6C(F)F)=N3

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6.4 mg/mL (14.37 mM; Need warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2448 mL 11.2241 mL 22.4482 mL
5 mM 0.4490 mL 2.2448 mL 4.4896 mL
10 mM 0.2245 mL 1.1224 mL 2.2448 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.67 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.67 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.67 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

The drug concentration causing 50% inhibition of cell proliferation (IC50) is obtained in lymphoma cell lines [diffuse large B cell lymphoma (DLBCL); mantle cell lymphoma (MCL); anaplastic large T-cell lymphoma; and others] exposed to increasing doses of PQR620 for 72 h using a Tecan D300e Digital Dispenser on 384 well plates[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]
For in vivo experiments, NOD-Scid (NOD.CB17-Prkdcscid/J) mice are subcutaneously inoculated with 10×106 (RIVA) or with 5×106(SU-DHL-6) cells. Treatments with PQR620 (100mg/kg dose per day, Qdx7/w) started with 100-150 mm3 tumors and are carried for 14 (SU-DHL-6) or 21 days (RIVA).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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PQR620
Cat. No.:
HY-100026
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