2. PI3K/Akt/mTOR
  3. PI3K
    mTOR
  4. Bimiralisib

Bimiralisib  (Synonyms: PQR309)

Cat. No.: HY-12868 Purity: 98.74%
COA Handling Instructions

Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.

For research use only. We do not sell to patients.

Bimiralisib Chemical Structure

Bimiralisib Chemical Structure

CAS No. : 1225037-39-7

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Based on 3 publication(s) in Google Scholar

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mTOR mTORC1 mTORC2

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.

IC50 & Target[1][2]

PI3Kα

33 nM (IC50)

PI3Kα-H1047R

36 nM (IC50)

PI3Kα-E542K

63 nM (IC50)

PI3Kα-E545K

136 nM (IC50)

PI3Kδ

451 nM (IC50)

PI3Kβ

661 nM (IC50)

PI3Kγ

708 nM (IC50)

Vps34

6486 nM (IC50)

mTOR

89 nM (IC50)

mTORC1

 

mTORC2

 

DNA-PK

8567 nM (IC50)

In Vitro

Bimiralisib is a highly selective pan-PI3K inhibitor with a balanced targeting of mTOR kinase. Bimiralisib also inhibits PI3Kα-H1047R), PI3Kα-E542K and PI3Kα-E545K with IC50s of 36 nM, 63 nM and 136 nM, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

Oral administration yields similar concentrations of Bimiralisib in brain and plasma samples illustrates that Bimiralisib readily passes the blood–brain barrier. In mice, 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, which reflects the time point when the drug 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. The half-life of 5-8 h and an AUC0.25-12 of around 14 000 h•ng/mL contributed to an excellent oral bioavailability of PQR309 (>50%). Twenty-four hours after po administration, plasma levels of PQR309 are still >2 μM (800-1000 ng/mL). Moreover, after 1-2 h exposure to PQR309 , drug levels in rat brain samples are comparable to plasma levels, confirming rapid access of PQR309 to the brain[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

411.38

Appearance

Solid

Formula

C17H20F3N7O2
CAS No.
SMILES

NC1=NC=C(C2=NC(N3CCOCC3)=NC(N4CCOCC4)=N2)C(C(F)(F)F)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (121.54 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4308 mL 12.1542 mL 24.3084 mL
5 mM 0.4862 mL 2.4308 mL 4.8617 mL
10 mM 0.2431 mL 1.2154 mL 2.4308 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.08 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.08 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.08 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
Cell Assay
[1]

Human tumor cell lines are seeded into 96-well microtiter plates and exposed to five (1/2 log serial) drug dilutions plus control, followed by 48 h (except for two controls of each cell line which are fixed with TCA (cell population at t =0 h [Tz]). The assay is terminated by fixation with TCA (10% final). Cell density is determined using a sulforhodamine B staining protocol and the absorbance measured at 515 nm. Using seven absorbance measurements, the percentage growth is calculated at each of the drug concentrations levels. Percentage growth inhibition is calculated. The NTRC Oncolines 44 cell lines are exposed for 72 h to 9-point 3-fold serial dilutions of Bimiralisib. The concentration of 50% growth inhibition is associated with the signal ((luminescenceuntreated,t=72h-luminescencet=0)/2)+luminescencet=0. The data set integrated here is used for IC50 calculations. IC50 values of A2058 or SKOV3 cell proliferation given are determined and calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Healthy male nude NIH rats are used. 2×107 PC-3 cells are injected subcutaneously at day 0 (D0) in 200 μL of RPMI1640 into the right flank of male nude rats, 24 h after a whole-body irradiation with a γ-source (5 Gy, 60Co). Tumor-bearing rats are randomized on day 16 (mean volume of 330±70 mm3 according to their individual tumor volume into five groups of each eight animals using Vivo manager software. Analysis of variance is performed to test for homogeneity between groups. Daily administration on D17-D44 and from D51 to D57: group 1, vehicle; group 2, compound 1 at 5 mg/kg; group 3, Bimiralisib at 10 mg/kg. Group 4: Bimiralisib at 15 mg/kg from D17 to D21, from D24 to D28, from D34 to D38, from D41 to D4, and from D51 to D56. Group 5: one iv injection of Vinorelbine at 2.5 mg/kg on D17, D24, D31, and D38. Final termination of rats is performed on D87. Body weight is measured at least twice a week. Length and width of tumors are measured and recorded twice a week with calipers, and the tumor volume is estimated.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Bimiralisib1225037-39-7PQR309PQR 309PQR-309PI3KmTORPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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