JAK/STAT Signaling

Dacomitinib (PF299804, PF299) (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.

Neratinib (HKI-272) (HKI-272) is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively.

Protein kinase inhibitor

EGFR inhibitor

Selective Mutated EGFR inhibitor

EGFR T790M inhibitor,irreversible amd potent

AST-1306 (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. AST-1306 also inhibits ErbB4 with an IC50 of 0.8 nM. AST-1306 is an anilino-quinazoline compound and has anti-cancer activity.

AEE788 (NVP-AEE788) is an inhibitor of the EGFR and ErbB2 with IC50 values of 2 and 6 nM, respectively.

Varlitinib (ARRY334543) (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively.

ARRY-380, an inhibitor of EGFR (ErbB1), is extracted from patent WO2015153959A2, compound 249. ARRY-380 is a potent, selective, ATP-competitive, orally active inhibitor of HER2.

GLPG0634 (GLPG0634) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.

Canertinib (CI-1033) is a potent and irreversible EGFR inhibitor that inhibits EGFR, HER2, and HER4 with IC 50 values of 0.8, 19, and 7nM, respectively.

HER2 inhibitor,potent and selective

AC480 (BMS-599626) (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. AC480 (BMS-599626) displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. AC480 (BMS-599626) inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.

AZD8931 (Sapitinib) (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.

AG-490 (Tyrphostin B42) is EGFR inhibitor with IC50 of 0.1 µM, AG-490 also has an inhibitory effect on JAK2.

Fludarabine is a purine analog that inhibits DNA synthesis.

Fludarabine (phosphate) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.

Mutant-selective EGFR inhibitor(L858R,T790M), irreversible and potent

AST-1306 TsOH (AST-1306 (TsOH)) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. AST-1306 TsOH also inhibits ErbB4 with an IC50 of 0.8 nM. AST-1306 TsOH is an anilino-quinazoline compound and has anti-cancer activity

AZD-9291 (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. AZD-9291 overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.

AZD-9291 mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.

AG-1478 is a selective EGFR tyrosine kinase inhibitor with IC 50 of 3nM.

AP26113 (Brigatinib analog) is a potent and selective active inhibitor of anaplastic lymphoma kinase(ALK), Patent US20140066406 A1.