BMF-219
目录号 : GC25159BMF-219是一种高选择性和不可逆的menin抑制剂,在小鼠模型中具有良好的抑制效果 。
Cas No.:2448172-22-1
Sample solution is provided at 25 µL, 10mM.
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BMF-219 is a highly selective and irreversible inhibitor of menin which has shown very promising activity in in-vitro and in-vivo preclinical tumour models[1-3].
BMF-219(6 or 24 hours; 0.5 or 1 µM) treatment significantly reduced MYC(v-myc avian myelocytomatosis viral oncogene homolog) transcription levels in cells[4].
BMF-219(40-200mg/kg; 28days; p.o) significantly reduces HbA1c and controls blood glucose levels in a 4-week dosing study in ZDF rats. BMF-219 significantly reduces blood lipemic levels and body weight in Streptozotocin (STZ) rats[5-6]. A comprehensive panel of Chronic Lymphocytic Leukemia (CLL) samples isolated from patients with Rai Stage 1 to 3 disease were cultured ex vivo in the presence of BMF-219 to assess the antileukemic activity. BMF-219 demonstrated high potency, achieving > 98% cell lethality at 1 µM exposure with IC50 values in the range of 0.1 to 0.38 µM[7].
References:
[1]. Dempke WCM, Desole M, et. al. Targeting the undruggable: menin inhibitors ante portas. J Cancer Res Clin Oncol. 2023 Sep;149(11):9451-9459. doi: 10.1007/s00432-023-04752-9. Epub 2023 Apr 27. PMID: 37103568.
[2]. Farhad Ravandi et al., COVALENT-101: A phase 1 study of BMF-219, a novel oral irreversible menin inhibitor, in patients with relapsed/refractory (R/R) acute leukemia (AL), diffuse large B-cell lymphoma (DLBCL), and multiple myeloma (MM). JCO 40, TPS7064-TPS7064(2022). DOI:10.1200/JCO.2022.40.16_suppl.TPS7064
[3]. JOSE E. RODRIGUEZ, et. al. 91-LB: COVALENT-111, a Phase 1/2 Trial of BMF-219, a Covalent Menin Inhibitor, in Patients with Type 2 Diabetes Mellitus—Preliminary Results. Diabetes 20 June 2023; 72 (Supplement_1): 91-LB. https://doi.org/10.2337/db23-91-LB
[4]. Priyanka Somanath, Daniel Lu,et. al. Novel Irreversible Menin Inhibitor, BMF-219, Shows Potent Single Agent Activity in Clinically Relevant DLBCL Cells. DOI: 10.1182/blood-2021-148045
[5]. PRIYANKA SOMANATH, et. al. 113-LB: Oral Menin Inhibitor, BMF-219, Displays a Significant and Durable Reduction in HbA1c in a Type 2 Diabetes Mellitus Rat Model. Diabetes 1 June 2022; 71 (Supplement_1): 113-LB. https://doi.org/10.2337/db22-113-LB
[6]. THOMAS BUTLER, et. al. 851-P: Oral Long-Acting Menin Inhibitor Normalizes Type 2 Diabetes Mellitus (T2DM) in Two Rat Models. Diabetes 1 June 2022; 71 (Supplement_1): 851-P. https://doi.org/10.2337/db22-851-P
[7]. Priyanka Somanath et al., Preclinical activity of irreversible Menin inhibitor, BMF-219, in chronic lymphocytic leukemia. JCO 40, 7541-7541(2022). DOI:10.1200/JCO.2022.40.16_suppl.7541
BMF-219是一种高选择性和不可逆的menin抑制剂,在小鼠模型中具有良好的抑制效果 [1-3]。
BMF-219(6 or 24 hours; 0.5 or 1 µM)治疗显著降低了细胞中MYC的转录水平[4]。
BMF-219(40-200mg/kg; 28days; p.o) 在为期4周的ZDF大鼠剂量研究中,显著降低HbA1c并控制血糖水平。BMF-219可显著降低链脲佐菌素(STZ)大鼠的血脂水平和体重[5-6]。从Rai 1至3期患者中分离的慢性淋巴细胞白血病(CLL)样本在体外存在BMF-219下培养,以评估其抗白血病活性。BMF-219表现出很高的效力,在1µM暴露下达到> 98%的细胞致死率,IC50值在0.1至0.38µM范围内[7]。
| Cell experiment [1]: | |
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Cell lines |
MOLM-13 cells |
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Preparation Method |
Cells incubated with BMF-219 for 6 and 24 hours at 0.5 µM and 1 µM. |
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Reaction Conditions |
6 or 24 hours; 0.5 or 1 µM |
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Applications |
BMF-219 treatment significantly reduced MYC(v-myc avian myelocytomatosis viral oncogene homolog) transcription levels in cells. |
| Animal experiment [2]: | |
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Animal models |
Zucker Diabetic Fatty (ZDF) rats |
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Preparation Method |
Rats were dosed daily with BMF-219 or vehicle for 28 days and monitored for an additional 28 days post last dose. |
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Dosage form |
40-200mg/kg; 28days; p.o |
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Applications |
BMF-219 dose groups showed improved glycemic control by oral glucose tolerance test (OGTT) on day 25. |
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References: [1]. Priyanka Somanath, Daniel Lu, et. al. Novel Irreversible Menin Inhibitor, BMF-219, Shows Potent Single Agent Activity in Clinically Relevant DLBCL Cells. DOI: 10.1182/blood-2021-148045 |
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| Cas No. | 2448172-22-1 | SDF | Download SDF |
| 分子式 | C31H34N8O3 | 分子量 | 566.65 |
| 溶解度 | 50mg/mL in DMSO (Need ultrasonic) | 储存条件 | Store at -20°C |
| 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 | 1.7648 mL | 8.8238 mL | 17.6476 mL |
| 5 mM | 0.353 mL | 1.7648 mL | 3.5295 mL |
| 10 mM | 0.1765 mL | 0.8824 mL | 1.7648 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet