S63845

SKU: orb1301867

Description

S63845 is a potent and selective small molecule inhibitor of myeloid cell leukemia 1 (MCL1), exhibiting high-affinity binding with a Kd of 0.19 nM. It is a valuable research tool for studying MCL1-dependent apoptosis in cancer models, including in vitro cell-based assays and in vivo studies of hematological malignancies.

Research Area

Cell Biology

Key Properties

• CAS Number: 1799633-27-4
• MW: 829.26
• Purity: 98.56%
• Formula: C₃₉H₃₇ClF₄N₆O₆S
• SMILES: CN1CCN(CCOc2ccc(-c3c(sc4ncnc(O[C@@H](Cc5ccccc5OCc5ccnn5CC(F)(F)F)C(O)=O)c34)-c3ccc(F)o3)c(C)c2Cl)CC1
• Target: Bcl-2 Family
• Solubility: DMSO:33.33 mg/mL (40.19 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (2.41 mM)

Bioactivity

• Target IC50:
  HuT78 cells:110 nM (EC50)|HCC1143 cells:3.1 ± 0.5 μM (EC50)|MDA-MB-468 cells:141.2 ± 24.7 nM (EC50)|MCL1:0.19 nM (Kd)|HH cells:22 nM (EC50)
• In Vivo:
  METHODS: S63845 (6.25, 12.5, 25 mg/kg, intravenous injection) was used to treat immunocompromised mice bearing human multiple myeloma (H929 and AMO1) xenografts, and its antitumor activity was observed. RESULTS S63845 showed dose-dependent antitumor activity; the maximum tumor growth inhibition (TGImax) was 114% in the AMO1 model and 103% in the H929 model.
• In Vitro:
  METHODS: HCT-116 cells were treated with S63845 (0.001-10 μM), and the levels of MCL1 and BCL-XL proteins in the cells were analyzed by Western blot. RESULTS S63845 effectively increased the level of MCL1 protein in the HCT-116 colon cancer cell line, but had no effect on the level of BCL-XL protein. The increase in MCL1 protein level was not accompanied by an increase in MCL1 mRNA level, but was associated with a prolonged protein half-life.

Storage & Handling

• Storage: store at low temperature,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

Bcl-2 Family, Inhibitor, inhibit, MCL-1, S63845, S-63845, S 63845

Compound Identifiers

PubChem CID

129606903