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Chemical Structure : PQR309
CAS No.: 1225037-39-7
Catalog No.: PC-43268Not For Human Use, Lab Use Only.
PQR309 (Bimiralisib) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50 of 33, 451, 661, 708 and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $88 | In stock | |
| 10 mg | $128 | In stock | |
| 25 mg | $228 | In stock | |
| 50 mg | $388 | In stock | |
| 100 mg | Get quote |
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PQR309 (Bimiralisib) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50 of 33, 451, 661, 708 and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively.
PQR309 (Bimiralisib) also shows potent activity against PI3Kα E542K/E545K/H2047R mutants with IC50 of 63/136/36 nM, shows no significant activity for VPS34 and DNA-PK (IC50>8,000 nM).
PQR309 (Bimiralisib) inhibits cellular phosphorylation of PKB/Akt on Ser473 and ribosomal S6 on Ser235/236 in A2058 melanoma cells with IC50 of 139 and 205 nM, SKOV3 cell growth IC50 is 237 nM.
PQR309 (Bimiralisib) demonstrates efficiency in inhibiting proliferation in tumor cell lines and rat xenograft models.
| M.Wt | 411.3816 | |
| Formula | C17H20F3N7O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-Pyridinamine, 5-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)- |
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1. Beaufils F, et al. J Med Chem. 2017 Sep 14;60(17):7524-7538.
2. Tarantelli C, et al. Clin Cancer Res. 2018 Jan 1;24(1):120-129.
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