S55746 hydrochloride (BCL201 hydrochloride) is a potent, orally active and selective BCL-2 inhibitor, with a K i of 1.3 nM and a K d of 3.9 nM. S55746 hydrochloride (BCL201 hydrochloride) has antitumor activity with low toxicity In Vitro S55746 (0-1 μM) potently and selectively induces cell death. S55746 selectively induces apoptosis through BCL-2 inhibition in a BAX/BAK-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: H146 and RS4;11 cell lines. Concentration: 0, 0.1, 0.3 and 1 μM. Incubation Time: 72 hours. Result: Potently induced RS4;11 cell killing after 72 h of treatment with an IC 50 of 71.6 nM. In Vivo S55746 is a highly efficacious and well-tolerated (even at doses up to 300 mg/kg) orally active BCL-2 inhibitor . S55746 (20-100 mg/kg, p.o.) inhibits xenograft growth in RS4;11 and Toledo models time- and dose-dependently . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female SCID/beige mice implanted subcutaneously with 3×10 6 Toledo or RS4;11 . Dosage: 20, 50, 100 mg/kg. Administration: Oral gavage daily for 7 consecutive days. Result: Induced significant anti-tumor activity time- and dose-dependently. Animal Model: SCID/beige female mice with RS4;11 tumor xenografts . Dosage: 25 and 100 mg/kg. Administration: Single oral gavage treatment. Result: Did not induce platelet loss in vivo at 25 and 100 mg/kg. Form:Solid IC50& Target:Bcl-2 1.3 nM (Ki) Bcl-xL 520 nM (Ki) Bcl-2 3.9 nM (Kd) Bcl-xL 186 nM (Kd)
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S55746 hydrochloride
CAS number：1448525-91-4 molecular formula：C43H43ClN4O6
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| Chinese alias | S55746 盐酸盐 | ||
| English alias | BDBM177786 | S 055746 | s55746 | S-55746 | US9120791, Example 1 | 1448584-12-0 | S55746 (BLC201) | S55746 (S 055746,BCL201) | (S)-N-(4-hydroxyphenyl)-3-(6-(3-(morpholinomethyl)-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)benzo[d][1,3]dioxol-5-yl)-N-phenyl-5 | ||
| CAS number | 1448525-91-4 | molecular formula | C43H43ClN4O6 |
| molecular weight | 747.28 g/mol | Exact mass | ≥98% |
| PSA | 96.700 Ų | logp | 5.800 |
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