1225037-39-7
PQR309
CAS: 1225037-39-7
Molecular Formula: C17H20F3N7O2
1225037-39-7 - Names and Identifiers
1225037-39-7 - Physico-chemical Properties
| Molecular Formula | C17H20F3N7O2 |
| Molar Mass | 411.38 |
| Density | 1.418±0.06 g/cm3(Predicted) |
| Boling Point | 643.7±65.0 °C(Predicted) |
| Solubility | 10 mM in DMSO |
| pKa | 4.92±0.10(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | In the vast majority of the lymphoma cell lines tested, PQR309 had potent activity with a mean IC50 of 233 nM(95% CI, 174-324 nmol/L). The arrest of cell proliferation is mainly due to cell cycle arrest, which blocks cells in the G1 phase rather than through the apoptotic pathway. PQR309 is more active in B- cell lymphoma cells such as DLBCL, MCL, CLL and SMZL than in T-cell derived ALCL. In lymphoma cell lines, PQR309 inhibits PI3K/mTOR signaling. PQR309 has anti-lymphoma activity in vitro and in vivo, whether administered as a single agent or in combination with other drugs. |
| In vivo study | In mice, rats and dogs, PQR309 has oral bioactivity, can cross the blood-brain barrier and has good pharmacokinetic parameters. PQR309 had only minimal clearance when exposed to rat, dog and human liver microsomes. In contrast, PQR309 was rapidly renewed in mouse liver microsomes, and 40% of the compound was cleared within 30 minutes. In female mice, the plasma concentration of PQR309 depends on the route of drug administration: the drug Half-Life is about 13-36 minutes for the oral route of administration and 9-10 minutes for the intravenous route. PQR309 has good oral bioavailability (>50%). Male beagle dogs were given oral administration of 10 mg/kg of the drug, and reached a peak plasma concentration (Cmax) of 583 ng/ml in 60-90 minutes after administration, with a half-life of more than 7 hours, the plasma concentration was about 150 ng/ml after 24 hours. The oral bioavailability of PQR309 in male beagle dogs was 23%. In all three animal models (Sprague-Dawley rat, CD-1 mouse, and Beagle dog),PQR309 was rapidly absorbed with good oral bioavailability. PQR309 has anti-proliferative activity in both PC3 prostate cancer cells and rat PC3 xenograft models. |
1225037-39-7 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.431 ml | 12.154 ml | 24.308 ml |
| 5 mM | 0.486 ml | 2.431 ml | 4.862 ml |
| 10 mM | 0.243 ml | 1.215 ml | 2.431 ml |
| 5 mM | 0.049 ml | 0.243 ml | 0.486 ml |
Last Update：2024-01-02 23:10:35
1225037-39-7 - Reference Information
| biological activity | Bimiralisib (PQR309) is a new type of PI3K/mTOR dual inhibitor that can penetrate into the brain and has anti-lymphoma activity in vitro and in vivo. Compared with other PI3K-related lipid kinase, protein kinase and non-related targets, it has higher selectivity for PI3K/mTOR. |
| target | TargetValue PI3Kα (Cell-free say) 1.5 nM (KD) PI3Kβ (Cell-free say) 11 nM (KD) mTOR (Cell-free say) 12 nM (KD) PI3Kγ (Cell-free say) 25 nM (KD) PI3Kδ (Cell-free say) 25 nM (KD) |
| Target | Value |
| PI3Kα (Cell-free assay) | 1.5 nM(Kd) |
| PI3Kβ (Cell-free assay) | 11 nM(Kd) |
| mTOR (Cell-free assay) | 12 nM(Kd) |
| PI3Kγ (Cell-free assay) | 25 nM(Kd) |
| PI3Kδ (Cell-free assay) | 25 nM(Kd) |
| in vitro study | in most of the lymphoma cell lines detected, PQR309 has effective activity with an average IC50 of 233 nM(95% CI, 174-324 nmol/L). Its arrest of cell proliferation is mainly due to cell cycle arrest, which blocks cells in G1 phase, rather than through the apoptosis pathway. PQR309 is more active in B- cell lymphoma cells (such as DLBCL, MCL, CLL and SMZL) than in T-cell-derived ALCL. In lymphoma cell lines, PQR309 inhibited PI3K/mTOR signaling. PQR309 has anti-lymphoma activity in vitro and in vivo, whether given as a single agent or in combination with other drugs. |
| in vivo studies | in mice, rats and dogs, PQR309 has oral biological activity, can cross the blood-brain barrier and has good pharmacokinetic parameters. PQR309 had minimal clearance when exposed to rat, dog and human liver microsomes. However, PQR309 was updated quickly in mouse liver microsomes, and 40% compounds were eliminated within 30 minutes. In female mice, the plasma concentration of PQR309 depends on the route of drug administration: the drug half-life of the oral route of administration is about 13-36 minutes, and the drug half-life of the intravenous route is 9-10 minutes. PQR309 has good oral bioavailability (>50%). The male beagle was given 10 mg/kg orally, and the blood concentration peak (Cmax) was 583 ng/ml 60-90 minutes after administration, the half-life was more than 7 hours, and the blood concentration was about 150 ng/ml after 24 hours. PQR309 has an oral bioavailability of 23% in male beagles. In three animal models (Sprague-Dawley rats, CD-1 mice and Beagle dog),PQR309 can be quickly absorbed and has good oral bioavailability. PQR309 has anti-tumor proliferative activity in both PC3 prostate cancer cells and rat PC3 transplanted tumor models. |
Last Update：2024-04-09 02:00:01
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Product Name: PQR309 Visit Supplier Webpage Request for quotationCAS: 1225037-39-7
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Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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