MS1943

SKU: orb1308790

Description

MS1943

Research Area

Cell Biology, Epigenetics & Chromatin, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2225938-17-8
• MW: 718.93
• Purity: 95.82%
• Formula: C₄₂H₅₄N₈O₃
• SMILES: CC(C)n1ncc2c(cc(cc12)-c1ccc(nc1)N1CCN(CCNC(=O)CC23CC4CC(CC(C4)C2)C3)CC1)C(=O)NCc1c(C)cc(C)[nH]c1=O
• Target: Apoptosis,Histone Methyltransferase,PROTACs
• Solubility: DMSO:120 mg/mL (166.91 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (6.95 mM)

Bioactivity

• Target IC50:
  EZH2:120 nM
• In Vivo:
  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.MS1943 suppresses tumor growth.
• In Vitro:
  MS1943 inhibits cell growth (GI50 of 2.2 μM). MS1943 induces cell death in MDA-MB-468 cells. MS1943 effectively reduces EZH2 levels in BT549, HCC70 and MDA-MB-231 TNBC cells, as well as KARPAS-422 and SUDHL8 lymphoma cells and PNT2 non-cancerous prostate cells.

Storage & Handling

• Storage: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

breast, cytotoxic, degrader, cancer, Apoptosis, Histone Methyltransferase, HistoneMethyltransferase, Inhibitor, EZH2, inhibit, MS 1943, MS1943, MS-1943, methyltransferase, proliferation, TNBC, triple-negative

Compound Identifiers

PubChem CID

139211327