Bimiralisib (PQR309) 是一种有效的，可渗透脑的，PI3K/mTOR 抑制剂，抑制 PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ 和 mTOR，IC50 分别为 33 nM，451 nM，661 nM，708 nM 和 89 nM。Bimiralisib 是 mTORC1 和 mTORC2 抑制剂。
| 生物活性 |
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. |
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| IC50&Target |
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| 体外研究 |
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. |
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| 体内研究 |
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.
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| 分子式 |
C17H20F3N7O2
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| 分子量 |
411.38
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| CAS号 |
1225037-39-7
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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| 溶解性数据 |
In Vitro:
DMSO : ≥ 50 mg/mL (121.54 mM) * "≥" means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
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| 临床试验 |
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| 科研文献 |
纯度： 98%
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