BGT226 (NVP-BGT226 maleate) 是一种PI3K(针对PI3Kα，PI3Kβ，PI3Kγ的IC50分别是4 nM，63 nM，38 nM ) /mTOR双抑制剂，对人头颈癌细胞具有较强的生长抑制活性。
| 生物活性 | BGT226 (NVP-BGT226 maleate) is aPI3K(withIC50s of 4 nM, 63 nM and 38 nM forPI3Kα,PI3KβandPI3Kγ) /mTORdual inhibitor which displays potent growth-inhibitory activity against human head and neckcancercells[1][2]. |
| IC50& Target | PI3Kα 4 nM (IC50) | PI3Kβ 63 nM (IC50) | PI3Kγ 38 nM (IC50) | mTOR | Autophagy |
|
体外研究
(In Vitro) | BGT226 shows significant growth inhibition or signal blockage profiles compared with LY294002 and Rapamycin. BGT226 (10-10000 nM) inhibits FaDu and OECM1 cells growth with IC50s of 23.1±7.4 and 12.5±5.1 nM, respectively[2].
The expression levels of p-mTOR Ser2481 are decreased in BGT226-treated cell lines (200 nM; 24 hours) and both p-AKT Ser473 and p-mTOR Ser2448 are also decreased in BGT226-treated cell lines[2].
Cell Viability Assay[2] | Cell Line: | FaDu cells; OECM1 cells | | Concentration: | 10, 100, 1000, 10000 nM | | Incubation Time: | | | Result: | Inhibited FaDu and OECM1 cells growth with IC50s of 23.1±7.4 and 12.5±5.1 nM, respectively. |
Western Blot Analysis[2] | Cell Line: | FaDu cells; OECM1 cells | | Concentration: | 200 nM | | Incubation Time: | 24 hour | | Result: | p-mTOR Ser2481 expression levels decreased, and both p-AKT Ser473 and p-mTOR Ser2448 expression levels also decreased. |
|
体内研究
(In Vivo) | BGT226 (2.5 and 5 mg/kg; oral administration for 21 days in male athymic mice) causes 34.7% and 76.1% reduction of the tumor growth on day 21 compared with control[2].
| Animal Model: | Male athymic mice (strain BALB/cAnN.Cg-Foxn1nu/CrlNarl) with FaDu cell xenografted mouse model[2] | | Dosage: | 2.5 and 5 mg/kg | | Administration: | Oral administration; 21 days | | Result: | Caused 34.7% and 76.1% reduction of the tumor growth. |
|
| Clinical Trial | |
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(153.70 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.5370 mL | 7.6852 mL | 15.3704 mL | | 5 mM | 0.3074 mL | 1.5370 mL | 3.0741 mL | | 10 mM | 0.1537 mL | 0.7685 mL | 1.5370 mL |
*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。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 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
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (3.84 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.84 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (3.84 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (3.84 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (3.84 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.84 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
|
m.cnreagent.com