1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK

Abrocitinib (Synonyms: PF-04965842)

目录号: HY-107429 纯度: 98.11%
产品使用指南

Abrocitinib (PF-04965842) 是一种有效、可口服、选择性的 JAK1 抑制剂,对 JAK1 和 JAK2 的 IC50 值分别为 29 和 803 nM。Abrocitinib (PF-04965842) 可抑制 TYK2 的活性(IC50,1.253 μM) 和刺激后 STAT1,STAT3 和 STAT5 的磷酸化水平。可用于自身免疫症的研究。

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Abrocitinib Chemical Structure

Abrocitinib Chemical Structure

CAS No. : 1622902-68-4

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥3850 In-stock
5 mg ¥3500 In-stock
10 mg ¥5500 In-stock
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Description

Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease[1].

IC50 & Target[1]

JAK1

29 nM (IC50)

JAK2

803 nM (IC50)

Tyk2

1253 nM (IC50)

In Vitro

Abrocitinib (Compound 25) inhibits IFNα-stimulated phosphorylation of STAT3, IFN-stimulated phosphorylation of STAT1 in human whole blood (HWB), as well as pSTAT5 in CD34+ spiked into HWB (JAK2), with IC50s of 189, 163 nM, 7.178 μM, respectively[1].

In Vivo

Abrocitinib (Compound 25; 5, 15, 50 mg/kg, p.o., daily for 7 days) significantly reduces paw swelling in rat adjuvant-induced arthritis model[1].

Animal Model: Female Lewis rats (8−10 weeks old)[1]
Dosage: 5, 15, 50 mg/kg
Administration: P.O. daily for 7 days
Result: Obviously reduced paw swelling at all doses.
References
Molecular Weight

323.41

Formula

C₁₄H₂₁N₅O₂S

CAS No.

1622902-68-4

SMILES

CN([C@H]1C[C@@H](NS(CCC)(=O)=O)C1)C2=C3C(NC=C3)=NC=N2

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
Abrocitinib
目录号:
HY-107429
需求量:

Abrocitinib

Cat. No.: HY-107429