Abrocitinib (PF-04965842) | JAK1 inhibitor

Chemical Structure : PF-04965842

CAS No.: 1622902-68-4

PF-04965842 (Abrocitinib, PF 04965842, PF04965842)

Catalog No.: PC-60671Not For Human Use, Lab Use Only.

PF-04965842 (Abrocitinib, PF04965842) is a potent, selective, orally bioavailable JAK1 inhibitor with IC50 of 29 nM.

Packing	Price	Stock
5 mg	$158	In stock
10 mg	$248	In stock
25 mg	$428	In stock
50 mg	$728	In stock
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Biological Activity

PF-04965842 (Abrocitinib, PF04965842) is a potent, selective, orally bioavailable JAK1 inhibitor with IC50 of 29 nM.

PF-04965842 exhibits good selective inhibition profile for JAK1 versus other JAK family enzymes (IC50=803/>10,000/1250 nM for JAK2/JAK3/TYK2, respectively).

PF-04965842 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.

PF-04965842 (5, 15, 50 mg/kg, p.o.) demonstrates efficacy in a rat adjuvant-induced arthritis (rAIA) model.

Physicochemical Properties

M.Wt	323.415
Formula	C14H21N5O2S
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide

References

1. Vazquez ML, et al. J Med Chem. 2018 Jan 3. doi: 10.1021/acs.jmedchem.7b01598.

2. Schmieder GJ, et al. Br J Dermatol. 2017 Sep 26. doi: 10.1111/bjd.16004.

PF-04965842 (Abrocitinib, PF 04965842, PF04965842)

Biological Activity

Physicochemical Properties

References

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