myelofibrosis

Bomedemstat ditosylate (IMG-7289 ditosylate) is an orally active lysine-specific demethylase 1 (LSD1) inhibitor with antitumor activity that potentiates the response to PD-1 inhibition in a homozygous model of SCLC, inhibits cancer cell proliferation, and induces apoptosis. Bomedemstat ditosylate can be used to study myeloproliferative neoplasms and myelofibrosis.

AZD1480 is a novel ATP-competitive JAK2 inhibitor (IC50: 0.26 nM), selectivity act against Tyk2 and JAK3, and to a smaller extent against JAK1. AZD1480 has been used in trials studying the treatment of Solid Malignancies, Post-Polycythaemia Vera, Primary

TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others.

TL-895 is an ATP-competitive, and highly selective irreversible inhibitor of Bruton’s Tyrosine Kinase(BTK). TL-895 showed good potency with an IC50 of 1.5 nM and a Ki of 11.9 nM.

Momelotinib HCl is a JAK1/2 inhibitor, reducing anemia in myelofibrosis (MF) patients.

Pacritinib (SB1518) citrate effectively inhibits wild-type JAK2 (IC 50 =23 nM) and the JAK2 V617F mutant (IC 50 =19 nM). It also targets FLT3 (IC 50 =22 nM) and the FLT3 D835Y mutant (IC 50 =6 nM). This compound is utilized in the study of acute myeloid leukemia (AML) and myelofibrosis (MF) [1] [2] [3].

Pacritinib hydrochloride is a potent inhibitor of wild-type JAK2 (IC50: 23 nM) and the JAK2V617F mutant (IC50: 19 nM), and can be used in the study of acute myeloid leukaemia (AML) and myelofibrosis (MF).

Bomedemstat (IMG-7289) is an orally active, irreversible inhibitor of lysine-specific demethylase 1 (LSD1) that exhibits antineoplastic activities in mouse models of myeloproliferative neoplasms (MPNs), and can be used for research on acute myelogenous leukemia (AML) and myelofibrosis (MF) [1].

Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor, tested for efficacy and safety in a phase II trial in myelofibrosis.