PQR309 ( Bimiralisib;PQR-309;PQR 309 )

Catalog No. M10862 CAS No. 1225037-39-7

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Product Name

PQR309
Note

Research use only, not for human use.
Brief Description

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.
Description

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; 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); 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; demonstrates efficiency in inhibiting proliferation in tumor cell lines and rat xenograft models. Brain Cancer Phase 2 Clinical
Synonyms

Bimiralisib;PQR-309;PQR 309
Pathway

PI3K/Akt/mTOR signaling
Target

PI3K
Recptor

pPKB;pS6
Research Area

Cancer
Indication

Brain Cancer

CAS Number

1225037-39-7
Formula Weight

411.38
Molecular Formula

C17H20F3N7O2
Purity

>98% (HPLC)
Solubility

10 mM in DMSO
SMILES

C1COCCN1C2=NC(=NC(=N2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4
Chemical Name

2-Pyridinamine, 5-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)-

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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