JAK/STAT Signaling

Tyk2-IN-3 is a Tyk2 pseudokinase inhibitor, with an IC50 of 485 nM.

Tarloxotinib bromide (TH-4000) is an irreversible inhibitor prodrug of EGFR/HER2.

Tucatinib (Irbinitinib) (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.

Pyrotinib (SHR-1258) (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively.

TAS6417 (CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM.

Mogrol is a biometabolite of mogrosides, and acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.

An orally bioavailable inhibitor of STAT3

Ilginatinib (NS-018) (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).

Naquotinib mesylate (ASP8273) (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer properties.

PF-06459988 is an orally activity, irreversible and mutant-selective inhibitor of EGFR mutant forms. PF-06459988 demonstrates high potency and specificity to the T790M-containing double mutant EGFRs. PF-06459988 can be used for the research of cancer.

SH5-07 is a hydroxamic acid based Stat3 inhibitor with an IC50 of 3.9 μM in in vitro assay.

GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma.

Pyrotinib dimaleate (SHR-1258 dimaleate) (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively.

Ilginatinib maleate (NS-018 (maleate)) (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).

Naquotinib (ASP8273) (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

JAK1-IN-3, is a highly selective, orally active Janus kinase 1 (JAK1) inhibitor with an IC 50 value of 73nM.

Ilginatinib hydrochloride (NS-018 hydrochloride) (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).

Gusacitinib (ASN-002) (ASN-002) is an orally active and potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM. Gusacitinib (ASN-002) has anti-cancer activity in both solid and hematological tumor types.

JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM).

Epertinib (S-22611) (S-22611) is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib (S-22611) shows potent antitumor activity.

Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. HS-10296 hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). HS-10296 hydrochloride is used for the research of the non-small cell lung cancer.

Rociletinib hydrobromide (CO-1686 (hydrobromide)) (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

Alflutinib (Furmonertinib) mesylate is is a potent inhibitor of EGFR. Alflutinib (Furmonertinib) mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Alflutinib (Furmonertinib) mesylate has the potential for the research of cancer diseases, especially non-small cell lung cancer (NSCLC).