Bomedemstat hydrochloride
(Synonyms: IMG-7289 hydrochloride) 目录号 : GC65879
Bomedemstat (IMG-7289) hydrochloride 是一种具有口服活性和不可逆的 lysine-specific demethylase 1 (LSD1) 抑制剂。Bomedemstat hydrochloride 可以增加 H3K4 和 H3K9 的甲基化，然后改变基因表达。Bomedemstat hydrochloride 具有抗癌活性，可抑制癌细胞增殖并诱导细胞凋亡。
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis[1][2].
Bomedemstat selectively inhibits proliferation and induces apoptosis of Jak2V617F cells by concomitantly increasing expression and methylation of p53[1].
Bomedemstat (50 nM-1 μM; 96 h) enhances survival, induces apoptosis via BCL-XL and PUMA in a TP53-dependent manner, and leads to cell cycle arrest[1].
Apoptosis Analysis[1]
| Cell Line: | SET-2 cells |
| Concentration: | 50 nM, 100 nM, and 1 μM |
| Incubation Time: | 96 hours |
| Result: | Decreased levels of the antiapoptotic protein BCL-XL and increased levels of the pro-apoptotic protein PUMA. |
Bomedemstat treatment (oral gavage; 45 mg/kg; once daily; 56 d) normalizes or improves blood cell counts, reduces spleen volumes, restores normal splenic architecture, and reduces bone marrow fibrosis[1].
| Animal Model: | Mx-Jak2V617F mice[1] |
| Dosage: | 45 mg/kg |
| Administration: | Oral gavage; 45 mg/kg; once daily; 56 days |
| Result: | Reduced splenomegaly significantly with a few treated mice normalizing their spleen weight, the 56-day course led to partial restoration of lymph follicles and spleen architecture by histological examination. |
| Cas No. | SDF | Download SDF | |
| 别名 | IMG-7289 hydrochloride | ||
| 分子式 | C28H35ClFN7O2 | 分子量 | 556.07 |
| 溶解度 | DMSO : 250 mg/mL (449.58 mM; Need ultrasonic) | 储存条件 | Store at -20°C, away from moisture |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7983 mL | 8.9917 mL | 17.9833 mL |
| 5 mM | 0.3597 mL | 1.7983 mL | 3.5967 mL |
| 10 mM | 0.1798 mL | 0.8992 mL | 1.7983 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。