| Identification | Back Directory | [Name]
MS1943 | [CAS]
2225938-17-8 | [Synonyms]
MS1943
1,6-Dimethyl-2-aminomethyl-3-benzyloxypyridin-4(1H)-one
1H-Indazole-4-carboxamide, N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-[2-[(2-tricyclo[3.3.1.13,7]dec-1-ylacetyl)amino]ethyl]-1-piperazinyl]-3-pyridinyl]- | [Molecular Formula]
C42H54N8O3 | [MOL File]
2225938-17-8.mol | [Molecular Weight]
718.93 |
| Chemical Properties | Back Directory | [density ]
1.36±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
Soluble in DMSO:100.0(Max Conc. mg/mL);139.1(Max Conc. mM) | [form ]
A solid | [pka]
12.56±0.46(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
MS1943 is used in the preparation of heterocyclic compounds as EZH2 ligands and their compositions and methods for treating EZH2-mediated cancer. MS1943 itself significantly reduces EZH2 protein levels in numerous triple-negative breast cancer | [Biological Activity]
MS1943 is a potent and selective degrader of EZH2 (enhancer of zeste homolog 2) th at effectively reduces EZH2 levels in cells. MS1943 potently inhibits growth of multiple TNBC cells and in mice xenograft model. | [in vivo]
MS1943 (150 mg/kg body weight; i.p.; once daily for 36 days) suppresses tumor growth[1].
MS1943 induces apoptosis in the MDA-MB-468 xenograft model[1].
A single i.p. injection of MS1943 at 50 mg/kg body weight achieved a peak plasma concentration (Cmax) of 2.9 μM and resulted in plasma concentrations above its cellular IC50 value for ~2h. A single 150 mg/kg body weight p.o. dose achieved Cmax of 1.1 μM, but plasma concentrations were below the cellular IC50 value[1]. | Animal Model: | Eight-week-old female BALB/c nude mice (MDA-MB-468 xenografts)[1] | | Dosage: | 150 mg/kg body weight | | Administration: | i.p.; once daily for 36 days | | Result: | Suppresses tumor growth. |
| [IC 50]
EZH2 methyltransferase: 120 nM (IC50) |
|
| Company Name: |
DC Chemicals
|
| Tel: |
021-58447131 13564518121 |
| Website: |
http://m.approvedhomemanagement.com/ShowSupplierProductsList927327/0.htm |
| Company Name: |
Wuhan Topule
|
| Tel: |
+86-02787215551 +86-19945035818 |
| Website: |
http://www.topule.com/ |
|