[CAS NO. 1990504-72-7] Bomedemstat ditosylate
PRODUCTS SPECIFICATIONS [1990504-72-7]
DESCRIPTION [1990504-72-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 864.02 |
| Molecular Formula | C42H50FN7O8S2 |
| SMILES | O=C(N1CCN(CC1)C)[C@@H](NC(C2=CC=C(N3C=CN=N3)C=C2)=O)CCCN[C@H]4[C@@](C5=CC=C(C=C5)F)([H])C4.O=S(C6=CC=C(C)C=C6)(O)=O.O=S(C7=CC=C(C)C=C7)(O)=O |
Summary
Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 ( LSD1 ) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis [1] [2] .
In Vitro
Bomedemstat selectively inhibits proliferation and induces
apoptosis
of
Jak2
V617F
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]
.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
In Vivo
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] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Mx-Jak2 V617F 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. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT05597306 | Terrence J Bradley, MD|Imago BioSciences, Inc., a subsidiary of Merck & Co., Inc., (Rahway, New Jersey USA)|University of Miami |
Acute Myeloid Leukemia|Refractory Acute Myeloid Leukemia|Acute Myeloid Leukemia, in Relapse
|
November 19, 2022 | Phase 1 |
| NCT05191797 | University of Washington|National Cancer Institute (NCI)|Imago BioSciences, Inc., a subsidiary of Merck & Co., Inc., (Rahway, New Jersey USA) |
Extensive Stage Lung Small Cell Carcinoma|Limited Stage Lung Small Cell Carcinoma
|
April 11, 2022 | Phase 1|Phase 2 |
| NCT04081220 | The University of Texas Health Science Center at San Antonio|Imago BioSciences, Inc., a subsidiary of Merck & Co., Inc., (Rahway, New Jersey USA) |
Thrombocythemia, Essential
|
April 9, 2020 | Phase 2 |
| NCT05569538 | The University of Hong Kong|Imago BioSciences, Inc., a subsidiary of Merck & Co., Inc., (Rahway, New Jersey USA) |
Myelofibrosis
|
December 1, 2022 | Phase 2 |
| NCT04262141 | Terrence J Bradley, MD|Imago BioSciences, Inc., a subsidiary of Merck & Co., Inc., (Rahway, New Jersey USA)|University of Miami |
Essential Thrombocythemia|Polycythemia Vera
|
October 2, 2020 | Phase 2 |
| NCT04254978 | Imago BioSciences, Inc., a subsidiary of Merck & Co., Inc., (Rahway, New Jersey USA) |
Essential Thrombocythemia
|
September 8, 2020 | Phase 2 |
| NCT02842827 | Imago BioSciences, Inc., a subsidiary of Merck & Co., Inc., (Rahway, New Jersey USA) |
Acute Myeloid Leukemia|Myelodysplastic Syndrome
|
October 6, 2016 | Phase 1|Phase 2 |
| NCT05223920 | Imago BioSciences, Inc., a subsidiary of Merck & Co., Inc., (Rahway, New Jersey USA) |
Thrombocythemia, Essential|Primary Myelofibrosis
|
December 16, 2021 | Phase 2 |
| NCT03136185 | Imago BioSciences, Inc., a subsidiary of Merck & Co., Inc., (Rahway, New Jersey USA) |
Myelofibrosis|Post-polycythemia Vera Myelofibrosis (PPV-MF)|Post-essential Thrombocythemia Myelofibrosis (PET-MF)|Primary Myelofibrosis (PMF)
|
July 1, 2017 | Phase 2 |
| NCT05558696 | Imago BioSciences, Inc., a subsidiary of Merck & Co., Inc., (Rahway, New Jersey USA) |
Polycythemia Vera
|
September 15, 2023 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL ( 115.74 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.1574 mL | 5.7869 mL | 11.5738 mL |
| 5 mM | 0.2315 mL | 1.1574 mL | 2.3148 mL |
| 10 mM | 0.1157 mL | 0.5787 mL | 1.1574 mL |
References
