PF 06551600 malonate

Pricing Availability   Qty
说明: Potent and selective JAK3 inhibitor
化学名: 1-[(2S,5R)-2-Methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-2-propen-1-one malate
纯度: ≥98% (HPLC)
说明书
引用文献
评论 (1)
通路 (1)

生物活性 for PF 06551600 malonate

PF 06551600 malonate is a potent and selective JAK3 inhibitor (IC50 = 33.1 μM). Exhibits no significant activity against a panel of other kinases including JAK1, JAK2 and TYK2. Inhibits phosphorylation of STAT5, induced by IL-2, IL-4, IL-7 and IL-15. Suppresses Th1 and Th17 T-cell differentiation and function in vitro. Reduces paw swelling in a rat model of arthritis and reduces disease severity in a rat EAE model.

许可信息

Sold for research purposes under agreement from Pfizer Inc.

化合物库 for PF 06551600 malonate

PF 06651600 malonate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。

技术数据 for PF 06551600 malonate

分子量 389.41
公式 C15H19N5O.C3H4O4
储存 Store at +4°C
纯度 ≥98% (HPLC)
CAS Number 2140301-97-7
PubChem ID 124203830
InChI Key QMPMPSGDPRHZCG-VZXYPILPSA-N
Smiles C[C@H]1CC[C@@H](NC2=C3C=CNC3=NC=N2)CN1C(C=C)=O.OC(CC(O)=O)=O

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for PF 06551600 malonate

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
water 38.94 100
DMSO 38.94 100

制备储备液 for PF 06551600 malonate

以下数据基于产品分子量 389.41。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.57 mL 12.84 mL 25.68 mL
5 mM 0.51 mL 2.57 mL 5.14 mL
10 mM 0.26 mL 1.28 mL 2.57 mL
50 mM 0.05 mL 0.26 mL 0.51 mL

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产品说明书 for PF 06551600 malonate

参考文献 for PF 06551600 malonate

参考文献是支持产品生物活性的出版物。

Thorarensen et al (2017) Design of a Janus Kinase 3 (JAK3) specific inhibitor 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) allowing for the interrogation of JAK3 signaling in humans. J.Med.Chem. 60 1971 PMID: 28139931

Telliez et al (2016) Discovery of a JAK3-selective inhibitor: functional differentiation of JAK3-selective inhibition over pan-JAK or JAK1-selective inhibition. ACS Chem.Biol. 11 3442 PMID: 27791347


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关键词: PF 06651600 malonate, PF 06651600 malonate supplier, PF06651600, malonate, JAK3, kinase, inhibitors, inhibits, potent, selective, anti-inflammatory, JAK, 6506, Tocris Bioscience

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PF 06551600 malonate 的评论

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Works well for JAK inhibitor..
By Scott Scarneo on 08/07/2019
分析类型: In Vitro
种属: Human
细胞系/组织: THP-1 Cells

To test the effects of this inhibitor on TNF production in stimulated THP-1 cells.

review image

Pathways for PF 06551600 malonate

JAK-STAT Signaling Pathway

JAK-STAT Signaling Pathway

The JAK-STAT signaling pathway has several roles, including the control of cell proliferation and hematopoiesis. It is the main signal transduction cascade from cytokine receptors.