Fig. 1 · Structure

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Abrocitinib (PF-04965842)

Cat. No. A18318 CAS 1622902-68-4

JAK1 inhibitor

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.

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Biological Activity

Target & Activity

Target Activity Value
JAK1 IC50 29 nM
JAK2 IC50 803 nM
Tyk2 IC50 1253 nM

Cellular Effect

Cell Line Activity Value Description Reference
TF-1 IC50 1.4 μM Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay [PMID: 32462873]

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 1622902-68-4
Applications JAK1 inhibitor
Formula C14H21N5O2S
Molecular Weight 323.415
Synonyms PF04965842. PF 04965842; PF-04965842
SMILES
CN([C@H]1C[C@@H](NS(CCC)(=O)=O)C1)C2=C3C(NC=C3)=NC=N2

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 58 mg/mL (179.34 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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