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  3. Parsaclisib hydrochloride

Parsaclisib hydrochloride  (Synonyms: INCB050465 hydrochloride; IBI-376 hydrochloride)

目录号: HY-109068A
产品使用指南 技术支持

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。

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Parsaclisib hydrochloride Chemical Structure

Parsaclisib hydrochloride Chemical Structure

CAS No. : 1995889-48-9

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1 mg ¥1772
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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class 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 IC50 of 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].

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

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].

MCE 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[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+CD44high and CD8+CD44high T cells in both spleens and tumors.
Clinical Trial
分子量

469.34

同用名

INCB050465 hydrochloride; IBI-376 hydrochloride

Formula

C20H23Cl2FN6O2

CAS 号
性状

固体

颜色

White to off-white

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)

纯度 & 产品资料
参考文献

Parsaclisib hydrochloride 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HY-109068A
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