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Bomedemstat(IMG-7289)是一种口服活性、不可逆的赖氨酸特异性去甲基酶1(LSD1)抑制剂,在小鼠骨髓增生性肿瘤(MPNs)模型中显示活性。该化合物具有抗肿瘤作用,可用于急性髓系白血病(AML)和骨髓纤维化(MF)研究。
Bomedemstat(IMG-7289)是一种口服活性、不可逆的赖氨酸特异性去甲基酶1(LSD1)抑制剂,在小鼠骨髓增生性肿瘤(MPNs)模型中显示活性。该化合物具有抗肿瘤作用,可用于急性髓系白血病(AML)和骨髓纤维化(MF)研究。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 346 | In stock | |
5 mg | ¥ 826 | In stock | |
10 mg | ¥ 1,230 | In stock | |
25 mg | ¥ 1,980 | In stock | |
50 mg | ¥ 2,960 | In stock |
Bomedemstat 相关产品
产品描述 | 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. |
体外活性 | Bomedemstat (50 nM-1 μM, 96 小时) 处理SET-2 细胞,能够提高存活率,并且以 TP53 依赖的方式通过 BCL-XL 和 PUMA 诱导细胞凋亡,还会导致细胞周期停滞。[1] |
体内活性 | 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. |
别名 | IMG-7289, IMG7289 |
分子量 | 519.61 |
分子式 | 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 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
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