Parsaclisib hydrochloride (INCB050465 hydrochloride) 是一种有效，选择性和具有口服活性的PI3Kδ抑制剂，IC50值为 1 nM。Parsaclisib hydrochloride 相对于其他 PI3K I 类同工型的选择性约为 20000 倍。Parsaclisib hydrochloride 可用于研究复发或难治性 B 细胞恶性肿瘤。
| 生物活性 | Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor ofPI3Kδ, with anIC50of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over otherPI3Kclass I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies[1][2][3]. |
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体外研究
(In Vitro) | Parsaclisib (0.1-3000 nM; 4 d) inhibits proliferation of MCL and DLBCL cell lines[2].
Parsaclisib (0.1-1000 nM; 2 h) inhibits anti-IgM-induced pAKT (Ser473) in the Ramos Burkitt’s lymphoma cell line, with an IC50of 1 nM[2].
Parsaclisib inhibits the proliferation of human, dog, rat, and mouse primary B cells after activation of these receptors, with IC50s ranging from 0.2 to 1.7 nM[2].
Cell Proliferation Assay[2] | Cell Line: | Jeko-1, Mino, JVM2, Rec-1, Pfeiffer, SU-DHL-5, SU-DHL-6, WSU-NHL, SU-DHL-4, SU-DHL-8, and WILL-2 cells | | Concentration: | 0.1-3000 nM | | Incubation Time: | 4 days | | Result: | Resulted in a maximal inhibition of 70-90%, with IC50s of ≤10 nM in the four MCL cell lines.
Pfeiffer, SU-DHL-5, SU-DHL-6, and WSU-NHL were highly sensitive, with IC50s from 2 to 8 nM. |
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体内研究
(In Vivo) | Parsaclisib (10 mg/kg; oral gavage twice daily for 7-19 days) inhibits tumor growth in the BALB/c mice bearing the A20 murine lymphoma cells[2].
Parsaclisib (0.1-10 mg/kg; p.o. twice daily) slows Pfeiffer xenograft tumor growth in a dose-dependent manner. And Parsaclisib was well tolerated[2].
Parsaclisib (0.5-1 mg/kg; a single p.o.) inhibits pAKT (Ser473) in Pfeiffer subcutaneous mouse xenograft models[2].
| Animal Model: | Female BALB/c mice (5-9 weeks) were inoculated with A20 cells[2] | | Dosage: | 10 mg/kg | | Administration: | Oral gavage twice daily for 7-19 days | | Result: | Resulted in significant tumor growth inhibition (TGI).
Reduced the percentage of Tregs (CD4+CD25+FOXP3+) in tumors and spleens.
Increased the ratio of CD4+and CD8+T cells to Tregs in spleens and tumors.
Decreased the number of CD4+CD44highand CD8+CD44highT cells in both spleens and tumors. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| 溶解性数据 | In Vitro: DMSO : 240 mg/mL(511.36 mM;Need ultrasonic) H2O : 100 mg/mL(213.07 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.1307 mL | 10.6533 mL | 21.3065 mL | | 5 mM | 0.4261 mL | 2.1307 mL | 4.2613 mL | | 10 mM | 0.2131 mL | 1.0653 mL | 2.1307 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 (stored under nitrogen)。-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： PBS Solubility: 50 mg/mL (106.53 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 6 mg/mL (12.78 mM); Clear solution
此方案可获得 ≥ 6 mg/mL (12.78 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 60.0 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 6 mg/mL (12.78 mM); Clear solution
此方案可获得 ≥ 6 mg/mL (12.78 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 60.0 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。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 6 mg/mL (12.78 mM); Clear solution
此方案可获得 ≥ 6 mg/mL (12.78 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 60.0 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。
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