Parsaclisib INCB050465; IBI-376|cas:1426698-88-5|西域试剂

Parsaclisib INCB050465; IBI-376,99.31%

产品编号：Bellancom-109068| CAS NO：1426698-88-5| 分子式：C₂₀H₂₂ClFN₆O₂| 分子量：432.88

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货号	价格	库存与货期
Bellancom-109068	￥3900.00	杭州北京（现货）
Bellancom-109068	￥6300.00	杭州北京（现货）
Bellancom-109068	￥12000.00	杭州北京（现货）

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Parsaclisib INCB050465; IBI-376

产品介绍

Parsaclisib (INCB050465) 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 相对于其他 PI3K I 类同工型的选择性约为 20000 倍。Parsaclisib 可用于研究复发或难治性 B 细胞恶性肿瘤。

生物活性

Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC₅₀ of 1 nM at 1 mM ATP. Parsaclisib shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib can be used for the research of relapsed or refractory B-cell malignancies.

体外研究

Parsaclisib (0.1-3000 nM; 4 d) inhibits proliferation of MCL and DLBCL cell lines.
Parsaclisib (0.1-1000 nM; 2 h) inhibits anti-IgM-induced pAKT (Ser473) in the Ramos Burkitt’s lymphoma cell line, with an IC₅₀ of 1 nM.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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.

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.
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.
Parsaclisib (0.5-1 mg/kg; a single p.o.) inhibits pAKT (Ser473) in Pfeiffer subcutaneous mouse xenograft models.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/c mice (5-9 weeks) were inoculated with A20 cells
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⁺CD44^high and CD8⁺CD44^high T cells in both spleens and tumors.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/c mice (5-9 weeks) were inoculated with A20 cells
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⁺CD44^high and CD8⁺CD44^high T cells in both spleens and tumors.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/c mice (5-9 weeks) were inoculated with A20 cells
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⁺CD44^high and CD8⁺CD44^high T cells in both spleens and tumors.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (288.76 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3101 mL	11.5505 mL	23.1011 mL
5 mM	0.4620 mL	2.3101 mL	4.6202 mL
10 mM	0.2310 mL	1.1551 mL	2.3101 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution
2.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution
3.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.81 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.81 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
4.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.81 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.81 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
5.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.81 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.81 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。