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| Size | Price | Stock |
|---|---|---|
| 250mg | $1020 | Check With Us |
| 500mg | $1650 | Check With Us |
| 1g | $2475 | Check With Us |
: Cat #: V2864 CAS #: 1225037-39-7 Purity ≥ 98%
Description: Bimiralisib (also known as PQR-309; PI3K-IN-2) is an orally bioavailable, brain-penetrant, and balanced pan-inhibitor of PI3K/mTOR (phosphoinositide-3-kinase/mammalian target of rapamycin) with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively.
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| Molecular Weight (MW) | 411.38 |
|---|---|
| Molecular Formula | C17H20F3N7O2 |
| CAS No. | 1225037-39-7 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 10 mM in DMSOr |
| Water: N/Ar | |
| Ethanol: N/A | |
| SMILES Code | NC1=NC=C(C2=NC(N3CCOCC3)=NC(N4CCOCC4)=N2)C(C(F)(F)F)=C1 |
| Synonyms | Bimiralisib; PQR309; PQR-309; PQR309; PI3K-IN-2; PI3K IN-2 |
| Protocol | 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. |
|---|---|---|
| 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. |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.4308 mL | 12.1542 mL | 24.3084 mL | 48.6169 mL |
| 5mM | 0.4862 mL | 2.4308 mL | 4.8617 mL | 9.7234 mL |
| 10mM | 0.2431 mL | 1.2154 mL | 2.4308 mL | 4.8617 mL |
| 20mM | 0.1215 mL | 0.6077 mL | 1.2154 mL | 2.4308 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.