LGB-321 HCl

Description

LGB-321 is a potent and selective ATP-competitive small molecule inhibitor of PIM kinases (Pan-PIM kinase inhibitor). LGB321 is unique relative to previously described PIM inhibitors, in that it is active in PIM2 dependent cell lines. , a kinase that has proven difficult to inhibit in the cellular context. Consistent with its activity on all three PIM kinases, LGB321 inhibits proliferation of a number of cell lines derived from diverse hematological malignancies, including MM, AML, CML and B-Cell NHL. In vivo, LGB-321 is orally available, demonstrates efficacy in tumor xenografts and is well-tolerated within the therapeutic exposure range in mice. (source: Clin Cancer Res. 2014 Apr 1;20(7):1834-45 )

in vitro

GB321 is active on PIM2-dependent multiple myeloma cell lines, where it inhibits proliferation, mTOR-C1 signaling and phosphorylation of BAD. Broad cancer cell line profiling of LGB321 demonstrates limited activity in cell lines derived from solid tumors._x000D_ _x000D_ Reference: Clin Cancer Res. 2014 Apr 1;20(7):1834-45. https://pubmed.ncbi.nlm.nih.gov/24474669/

in vivo

Furthermore, this study demonstrates LGB321 activity in the KG-1 AML xenograft model, in which modulation of pharmacodynamics markers is predictive of efficacy. Finally, this study demonstrates that LGB321 synergizes with cytarabine in this model._x000D_ _x000D_ Reference: Clin Cancer Res. 2014 Apr 1;20(7):1834-45. https://pubmed.ncbi.nlm.nih.gov/24474669/

target

LGB-321 is a potent and selective ATP-competitive small molecule inhibitor of PIM kinases (Pan-PIM kinase inhibitor).

Raw materials

Preparation Products