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Bomedemstat (IMG-7289), an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor, shows activity in mouse myeloproliferative neoplasm (MPN) models. This compound exhibits antineoplastic effects and can be used for acute myeloid leukemia (AML) and myelofibrosis (MF) research.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $67 | In Stock | |
5 mg | $162 | In Stock | |
10 mg | $243 | In Stock | |
25 mg | $411 | In Stock | |
50 mg | $598 | In Stock | |
100 mg | $848 | In Stock |
Description | Bomedemstat (IMG-7289), an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor, shows activity in mouse myeloproliferative neoplasm (MPN) models. This compound exhibits antineoplastic effects and can be used for acute myeloid leukemia (AML) and myelofibrosis (MF) research. |
In vitro | Bomedemstat (50 nM-1 μM, 96 hours) treatment of SET-2 cells increases survival and induces apoptosis via BCL-XL and PUMA in a TP53-dependent manner, leading to cell cycle arrest. [1] |
In vivo | Once-daily treatment with IMG-7289 normalized or improved blood cell counts, reduced spleen volumes, restored normal splenic architecture, and reduced bone marrow fibrosis. Most importantly, LSD1 inhibition lowered mutant allele burden and improved survival [1]. Animal Model: Mx1cre-Jak2 V617F 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. |
Synonyms | IMG-7289, IMG7289 |
Molecular Weight | 519.61 |
Formula | C28H34FN7O2 |
Cas No. | 1990504-34-1 |
Smiles | N(CCC[C@@H](C(=O)N1CCN(C)CC1)NC(=O)C2=CC=C(C=C2)N3C=CN=N3)[C@H]4[C@@H](C4)C5=CC=C(F)C=C5 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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