Bomedemstat ditosylate
Modify Date: 2024-01-10 16:27:22
Bomedemstat ditosylate structure
|
Common Name | Bomedemstat ditosylate | ||
|---|---|---|---|---|
| CAS Number | 1990504-72-7 | Molecular Weight | 864.02 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C42H50FN7O8S2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Bomedemstat ditosylateBomedemstat (IMG-7289) ditosylate is an oral and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity[1]. |
| Name | Bomedemstat ditosylate |
|---|
| Description | Bomedemstat (IMG-7289) ditosylate is an oral and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity[1]. |
|---|---|
| Related Catalog | |
| In Vitro | Bomedemstat (IMG-7289) ditosylate selectively inhibits proliferation and induced apoptosis of JAK2V617F cells by concomitantly increasing expression and methylation of p53, and, independently, the pro-apoptotic factor PUMA and by decreasing the levels of its antiapoptotic antagonist BCL-XL[1]. Bomedemstat (25 nM, 50 nM) ditosylate and Ruxolitinib (175 nM) synergize in inhibiting JAK2V617F-driven proliferation[1]. Bomedemstat (50 and 100 nM) ditosylate exerts a pro-apoptotic effect on 3 key regulators of programmed cell death, TP53, BCL-XL, and PUMA[1]. Cell Viability Assay[1] Cell Line: The human cell lines SET-2 (ATCC 608) and HEK293 Concentration: 25 nM, 50 nM Incubation Time: 96 hours Result: 25 nM alone significantly reduced colony formation. Western Blot Analysis[1] Cell Line: SET-2 cells Concentration: 50 and 100 nM Incubation Time: Result: Decreased levels of the antiapoptotic protein BCL-XL and increased levels of the pro-apoptotic protein PUMA. |
| In Vivo | Once-daily treatment with Bomedemstat (IMG-7289; 45 mg/kg) ditosylate normalizes or improves blood cell counts, reduces spleen volumes, restores normal splenic architecture, and reduces bone marrow fibrosis[1]. Animal Model: Mx1cre-Jak2V617F mice[1] Dosage: 45 mg/kg Administration: Administered daily by oral gavage for either 14, 42, or 56 consecutive days Result: In this Mx-Jak2V617F model of myeloproliferative neoplasm (MPN), mice developed severe splenomegaly (up to 10-fold increase in spleen weight). Splenic architecture was completely destroyed, eliminating demarcation of the white and red pulp. Treatment significantly reduced splenomegaly with a few treated mice normalizing their spleen weight. Remarkably, the 56-day course led to partial restoration of lymph follicles and spleen architecture by histological examination. |
| References |
| Molecular Formula | C42H50FN7O8S2 |
|---|---|
| Molecular Weight | 864.02 |