[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
| MDL | MFCD31715456 |
|---|---|
| Molecular Weight | 710.82 |
| Molecular Formula | C43H42N4O6 |
| 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 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
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 mg | 5 mg | 10 mg | |
| 1 mM | 1.4068 mL | 7.0341 mL | 14.0683 mL |
| 5 mM | 0.2814 mL | 1.4068 mL | 2.8137 mL |
| 10 mM | 0.1407 mL | 0.7034 mL | 1.4068 mL |
| 50 mM | 0.0281 mL | 0.1407 mL | 0.2814 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.
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