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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. It also showing antitumor activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $29 | In Stock | |
5 mg | $68 | In Stock | |
10 mg | $98 | In Stock | |
25 mg | $197 | In Stock | |
50 mg | $293 | In Stock | |
100 mg | $428 | In Stock | |
1 mL x 10 mM (in DMSO) | $75 | In Stock |
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. It also showing antitumor activity. |
Targets&IC50 | PI3Kδ:11 nM (Kd), PI3KC2β:100 nM (Kd), PI3Kβ:6.1 nM (Kd), PI3Kα:0.84 nM (Kd), PI3Kγ:10 nM (Kd), mTOR:0.33 nM (Kd) |
In vitro | PQR-530 inhibits all PI3K isoforms and mTOR complexes C1/2 potently and selectively. PQR-530 inhibits protein kinase B (PKB, pSer473) and ribosomal protein S6 (pS6, pSer235/236) phosphorylation (IC50: 0.07 μM in A2058 melanoma cells). PQR-530 displays inhibitory activity against the growth of 44 cancer cell lines (mean GI50: 426 nM)[1]. |
Alias | PQR-530 |
Molecular Weight | 407.42 |
Formula | C18H23F2N7O2 |
Cas No. | 1927857-61-1 |
Smiles | C[C@H]1COCCN1c1nc(nc(n1)-c1cnc(N)cc1C(F)F)N1CCOCC1 |
Relative Density. | 1.338 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 25 mg/mL (61.36 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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