| Company Name: |
BOC Sciences |
| Tel: |
1-631-485-4226; 16314854226 |
| Email: |
info@bocsci.com |
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| | LGB-321 HCl Basic information |
| | LGB-321 HCl Chemical Properties |
| | LGB-321 HCl Usage And Synthesis |
| 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_
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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_
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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). |
| | LGB-321 HCl Preparation Products And Raw materials |
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