S63845 [1799633-27-4]

Catalog number: HY-100741_100mg
Brand: MedChem Express
Packing: 100 mg
Other sizes: 5 mg
10 mM
25 mg
50 mg
Price: € 1396.00
Expected delivery time: 10 days

Product specifications for - S63845 [1799633-27-4]

Product group: Chemicals
Category: Other
CAS No.: 1799633-27-4
Purity: >98%
Molecular Formula: C39H37ClF4N6O6S
Molecular weight: 829.26
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor, binds human MCL1 with a Kd of 0.19 nM. IC50 & Target: Kd: 0.19 nM (MCL1)[1] In Vitro: The pro-survival protein myeloid cell leukemia 1 (MCL1) is over expressed in many cancers. S63845 is a small molecule that specifically binds with high affinity to the BH3-binding groove of MCL1. S63845 potently kills MCL1-dependent cancer cells, including multiple myeloma, leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway. The activity of S63845 is next evaluated in a panel of eight AML cell lines: all lines are sensitive to S63845 (IC50=4-233 nM)[1]. In Vivo: S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. Intravenously injected (i.v.) S63845 exerts dose-dependent anti-tumour activity in human multiple myeloma (H929 and AMO1) xenografts in immunocompromised mice, with maximal tumour growth inhibition of 114% in the AMO1 model and 103% in the H929 model. At 25 mg/kg, S63845 induces complete regression in 7 out of 8 of the mice at 100 days after treatment in the AMO1 model[1].
Safety information: