BMF-219 |
Catalog No.GC25159
One-Click Copy Product Info
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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.
Products are for research use only. Not for human use. We do not sell to patients.
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
| 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 | |
| Formula | C31H34N8O3 | M.Wt | 566.65 |
| Solubility | 50mg/mL in DMSO (Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7648 mL | 8.8238 mL | 17.6476 mL |
| 5 mM | 353 μL | 1.7648 mL | 3.5295 mL |
| 10 mM | 176.5 μL | 882.4 μL | 1.7648 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)