Size | Price | Stock | Qty |
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2mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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Purity: ≥98%
PQR620 is a novel, potent, selective and brain penetrant inhibitor of mTORC1/2 which plays a fundamental role in cell proliferation, differentiation, growth and survival.In lymphomas, the PI3K/AKT/mTOR pathway is a crucial therapeutic target. PQR309 is a dual PI3K/mTOR inhibitor that is in a phase 2 trial (NCT02249429, NCT02723877, NCT02669511) and has demonstrated in vitro anti-lymphoma activity. In solid tumor models, the novel mTORC1/2 inhibitor PQR620 has demonstrated preclinical activity (Beaufils et al., AACR 2016). The novel mTORC1/2 inhibitor PQR620 demonstrated both in vitro and in vivo anti-lymphoma activity. In vivo tests revealed that the PI3K/mTOR dual inhibitor PQR309 and PQR620 can both benefit significantly from the addition of the BCL2 inhibitor venetoclax.
Targets |
TORC1 (IC50 = 250 nM); TORC2 (IC50 = 250 nM)
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ln Vitro |
PQR620 is a novel brain penetrant dual TORC1/2 inhibitor that exhibits anti-tumor activity in 56 lymphoma cell lines and has a median IC50 value of 250 nM after 72 hours of exposure.[1]
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ln Vivo |
PQR620 exhibits anti-lymphoma activity in vivo and interacts synergistically with venetoclax, a BCL2 inhibitor. In a xenograft model of GCB-DLBCL, the combination of PQR620 and venetoclax has greater in vivo anti-tumor activity than either drug alone. [1]
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Cell Assay |
PQR620 is dissolved in dimethyl sulphoxide (DMSO) to obtain a stock concentration of 10 mM. PQR620 is examined in a sizable panel of lymphoma-derived cell lines (n = 56). 2 mM PQR620 is applied to cell lines for 24 hours, with DMSO serving as the control.
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Animal Protocol |
Mice:
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).
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References |
Molecular Formula |
C21H25F2N7O2
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Molecular Weight |
445.47
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Exact Mass |
445.2038
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Elemental Analysis |
C, 56.62; H, 5.66; F, 8.53; N, 22.01; O, 7.18
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CAS # |
1927857-56-4
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Appearance |
Solid powder
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SMILES |
C1C[C@H]2COC[C@@H]1N2C3=NC(=NC(=N3)C4=CN=C(C=C4C(F)F)N)N5[C@@H]6CC[C@H]5COC6
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InChi Key |
UGDKPWVVBKHRDK-KPWCQOOUSA-N
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InChi Code |
InChI=1S/C21H25F2N7O2/c22-18(23)15-5-17(24)25-6-16(15)19-26-20(29-11-1-2-12(29)8-31-7-11)28-21(27-19)30-13-3-4-14(30)10-32-9-13/h5-6,11-14,18H,1-4,7-10H2,(H2,24,25)/t11-,12+,13-,14+
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Chemical Name |
5-[4,6-bis[(1R,5S)-3-oxa-8-azabicyclo[3.2.1]octan-8-yl]-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.