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| Cas No.: | 1448525-91-4 |
| SMILES: | O=C(C1=C2CCCCN2C(C3=C(C(N4CC5=C(C=CC=C5)C[C@H]4CN6CCOCC6)=O)C=C(OCO7)C7=C3)=C1)N(C8=CC=C(O)C=C8)C9=CC=CC=C9.Cl |
| Formula: | C43H43ClN4O6 |
| M.Wt: | 747.28 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | In Vitro S55746 hydrochloride is a potent, orally active and selective BCL-2 inhibitor, with Kis and Kds of 1.3 nM, 520 nM and 3.9 nM, 186 nM for BCL-2 and BCL-XL, respectively. S55746 selectively induces cell death. S55746 potently causes RS4;11 cell killing with an IC50 of 71.6 nM after 72 h of treatment, but shows a much weaker activity in H146 (IC50 1.7 μM), a BCL-XL-dependent cell line. S55746 also selectively induces apoptosis through BCL-2 inhibition in a BAX/BAK-dependent manner. S55746 (3 nM) induces cell death in CLL cells. In Vivo S55746 is a highly efficacious and well-tolerated orally active BCL-2 inhibitor. S55746 (25 and 100 mg/kg, p.o.) inhibits xenograft growth in RS4;11 and Toledo models. |