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S55746 hydrochloride

Chemical Structure : S55746 hydrochloride

CAS No.: 1448525-91-4

S55746 hydrochloride (BCL201;BCL-201;S 55746;S-55746;Servier-1)

Catalog No.: PC-63501Not For Human Use, Lab Use Only.

S55746 (BCL201, Servier-1) hydrochloride is a novel potent, selective, orally bioavailable inhibitor of BCL-2 with Ki of 1.3 nM, 70- 400 fold selectivity over BCL-XL, on significant binding to MCL-1 and BFL-1.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

S55746 (BCL201, Servier-1) hydrochloride is a novel potent, selective, orally bioavailable inhibitor of BCL-2 with Ki of 1.3 nM, 70- 400 fold selectivity over BCL-XL, on significant binding to MCL-1 and BFL-1.
S55746 potently induces RS4;11 cell killing after 72 h of treatment with an IC50 of 71.6 nM, exhibits a much weaker activity in H146 (IC50 1.7 μM), a BCL-XL-dependent cell line.
S55746 concentration-dependently disrupts the BCL-2/BAX complex in RS4;11 cells, selectively induces apoptosis through BCL-2 inhibition in a BAX/BAK-dependent manner.
S55746 induces cell death in a panel of non-Hodgkin lymphoma cells; inhibits xenograft growth in RS4;11 and Toledo models.

Physicochemical Properties

M.Wt 747.289
Formula C43H43ClN4O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-Hydroxyphenyl)-3-[6-[(3S)-3-(morpholinomethyl)-3,4-dihydro-1H-isoquinoline2-carbonyl]-1,3-benzodioxol-5-yl]-N-phenyl-5,6,7,8-tetrahydroindolizine-1-carboxamide hydrochloride

References

1. Casara P, et al. Oncotarget. 2018 Apr 13;9(28):20075-20088.

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