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Cat. No. Product Name CAS No. Information
PC-61986

AZD 4205

2091134-68-6

AZD 4205 (AZD4205) is a potent, selective JAK1 inhibitor IC50 of 73 nM and Ki of 2.8 nM, shows high selectivity against JAK2 and JAK3 with IC50 of 13,233 nM and >30,000 nM respectively; shows potent inhibition of p-STAT3 in a cell based assay of JAK1 activity with an IC50 of 128 nM and excellent selectivity across the kinome; reduces residual disease and prolongs the benefit of Osimertinib in lung cancer patients with EGFR activating mutations both in vitro and in vivo.

Lung Cancer

Phase 2 Clinical

PC-60988

AS 2553627

1251906-07-6

AS 2553627 (AS2553627) is a novel potent, selective pan-JAK inhibitor with IC50 of 0.46, 0.30, 0.14 and 2.0 nM for JAK1, JAK2, JAK3 and TYK2, respectively; displays no inhibitory activity against a panel of protein kinases, including SYK and ZAP70 at 1 uM; inhibits proliferation of IL-2 stimulated human and rat T cells with IC50 of 2.4 and 4.3 nM, respectively, inhibits the proliferation of TF-1 cells stimulated with EPO with IC50 of 12 nM; effectively prevents chronic rejection in rat cardiac allografts in rat cardiac transplant model alone or co-administration with tacrolimus.

PC-60671

PF-04965842

1622902-68-4

PF-04965842(PF04965842) is a potent, selective, orally bioavailable JAK1 inhibitor with IC50 of 29 nM; exhibits good selective inhibition profile for JAK1 versus other JAK family enzymes (IC50=803/>10,000/1250 nM for JAK2/JAK3/TYK2, respectively); demonstrates efficacy in a rat adjuvant-induced arthritis (rAIA) model.

Dermatitis

Phase 3 Clinical

PC-60508

Delgocitinib

1263774-59-9
Delgocitinib (JTE-052, LEO 124249) is a potent, selective, orally active, pan-JAK inhibitor with IC50 of 2.8, 2.6, 13 and 58 nM for JAK1,2,3 and Tyk2, respectively; does not inhibit a broad panel of kinases with exception of ROCK-II (IC50=140 nM); inhibits cytokine signaling evoked by IL-2, IL-6, IL-23, granulocyte/macrophage CSF, and IFN-α in vitro; potently suppresses the IL-2-induced IFN-γ production in mice (ED50=1.1 mg/kg), suppresses inflammatory responses in collagen-induced arthritis model.
 
Psoriasis
 
Phase 2 Clinical
PC-60312

PF-06263276

1421502-62-6

PF-06263276 (PF06263276, PF 6263276) is a potent, selective pan JAK inhibitor with IC50 of 2.2, 23.1, 59.9 and 29.7 nM for JAK1, JAK2, JAK3, and TYK2, respectively; demonstrates good JAK potency and kinase selectivity, exhibts inhibitory potency in human whole blood versus various stimulatory cytokines (IFNα, IL-23, IL-4, IL-6 and GM-CSF) with IC50 of 0.6-5.2 uM; suitable for inhaled and topical delivery in vivo.

Psoriasis

Phase 1 Discontinued

PC-45653

Upadacitinib

1310726-60-3

Upadacitinib (ABT-494) is a potent and selective JAK1 inhibitor with celluar IC50 of 8 nM, biochemical IC50 of 40 nM; displays 74-fold and 50-fold selectivity over JAK2 and JAK3, respectively; a second-generation JAK inhibitor in development for rheumatoid arthritis.

Rheumatoid Arthritis

Phase 3 Clinical

PC-45652

Peficitinib

944118-01-8

Peficitinib (ASP-015K, JNJ-54781532) is a potent JAK inhibitor with IC50s of 3.9 and 0.7 nM for JAK1 and JAK3 respectively; inhibits IL-2-dependent T cell proliferation in vitro and STAT5 phosphorylation in vitro and ex vivo; dose-dependently suppresses bone destruction and paw swelling in an adjuvant-induced arthritis model in rats; orally bioactive.

Rheumatoid Arthritis

Phase 3 Clinical

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