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Parsaclisib hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Parsaclisib hydrochloride图片
CAS NO:1995889-48-9
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
INCB050465 hydrochloride
产品介绍
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].

IC50& Target[1]

PI3Kδ

1 nM (IC50)

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.
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.
Clinical Trial
分子量

469.34

性状

Solid

Formula

C20H23Cl2FN6O2

CAS 号

1995889-48-9

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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1307 mL10.6533 mL21.3065 mL
5 mM0.4261 mL2.1307 mL4.2613 mL
10 mM0.2131 mL1.0653 mL2.1307 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。

    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
  • 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。

    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
  • 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。