[CAS NO. 1448584-12-0]  S55746

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PRODUCTS SPECIFICATIONS [1448584-12-0]

Catelog
SLK-S8759
Brand
Selleck
CAS
1448584-12-0

DESCRIPTION [1448584-12-0]

Overview

MDLMFCD31715456
Molecular Weight710.82
Molecular FormulaC43H42N4O6
SMILESO=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

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.4068 mL7.0341 mL14.0683 mL
5 mM0.2814 mL1.4068 mL2.8137 mL
10 mM0.1407 mL0.7034 mL1.4068 mL
50 mM0.0281 mL0.1407 mL0.2814 mL

Description

S55746 (S 055746,BCL201) is a novel, orally active specific inhibitor (Ki = 1.3 nM) with poor affinity for BCL-XL and no significant binding to MCL-1, BFL-1 (BCL2A1/A1). The selectivity of S55746 for BCL-2 versus BCL-XL ranges from ~70 to 400 folds.

Targets

Bcl-2 [1]
(Cell-free assay)
1.3 nM(Ki)

In vitro

S55746 occupies the hydrophobic groove of BCL-2. In a panel of hematological cell lines, S55746 induces hallmarks of apoptosis including externalization of phosphatidylserine, caspase-3 activation and PARP cleavage. S55746 potently induces RS4;11 cell killing after 72 h of treatment with an IC50 of 71.6 nM and exhibits a much weaker activity in H146 (IC50 = 1.7 μM), a BCL-XL-dependent cell line, which expresses a low level of BCL-2 and high level of BCL-XL. It has no cytotoxic activity on BCL-XL-dependent cells, such as platelets.