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Bimiralisib

Cat. No. M9017
Bimiralisib Structure
Synonym:

PQR309; Bimiralisib free base

Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 200 In stock
25mg USD 400 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor, Bimiralisib inhibits PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM, respectively. PQR309 also inhibits PI3Kα-H1047R, PI3Kα-E542K and PI3Kα-E545K with IC50s of 36 nM, 63 nM and 136 nM, respectively. In vivo, both po and iv application routes show a rapid drop below 200 ng/mL (~0.5 μM) of PQR309 within <1 h (iv) to <2 h (po) after administration in mice, which reflects the time point when the compound reaches the median GI50 determined in tumor cell lines. In female rats a single oral dose (10 mg/kg) achieves similar drug levels as a single intravenous injection (5 mg/kg) with regard to Cmax.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 411.38
Formula C17H20F3N7O2
CAS Number 1225037-39-7
Purity >98%
Solubility DMSO: 10 mM
Storage at -20°C
References

First-in human, phase 1, dose-escalation pharmacokinetic and pharmacodynamic study of the oral dual PI3K and mTORC1/2 inhibitor PQR309 in patients with advanced solid tumors (SAKK 67/13).
Wicki A, et al. Eur J Cancer. 2018 Jun;96:6-16. PMID: 29660598.

5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.
Beaufils F, et al. J Med Chem. 2017 Sep 14;60(17):7524-7538. PMID: 28829592.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Bimiralisib, PQR309; Bimiralisib free base supplier, PI3K, inhibitors

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