[CAS NO. 1235034-55-5] A-1155463
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PRODUCTS SPECIFICATIONS [1235034-55-5]
Catalog
SLK-S7800
Brand
Selleck
CAS
1235034-55-5
DESCRIPTION [1235034-55-5]
Overview
| MDL | MFCD29924714 |
|---|---|
| Molecular Weight | 669.79 |
| Molecular Formula | C35H32FN5O4S2 |
| SMILES | O=C(C1=C(CCCOC2=CC=C(C#CCN(C)C)C=C2F)SC(N3CC4=C(C=CC=C4C(NC5=NC6=CC=CC=C6S5)=O)CC3)=N1)O |
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 | 1.4930 mL | 7.4650 mL | 14.9301 mL |
| 5 mM | 0.2986 mL | 1.4930 mL | 2.9860 mL |
| 10 mM | 0.1493 mL | 0.7465 mL | 1.4930 mL |
| 50 mM | 0.0299 mL | 0.1493 mL | 0.2986 mL |
Description
A-1155463, a highly potent and selective inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM).
Targets
| BCL-XL [1] (Cell-free assay) |
| <0.01 nM(Ki) |
In vitro
A-1155463 disrupts BCL-XL-BIM but not BCL-2-BIM complexes in cells. A-1155463 kills BCL-XL-dependent Molt-4 cells (EC50=70 nM) but has no measurable cytotoxicity against BCL-2-dependent RS4;11 cells
(EC50>5 mM). A-1155463 induces the hallmarks of apoptosis, as evidenced by the release of cytochrome c from mitochondria, caspase activation, and the accumulation of caspase-dependent sub-G0-G1 DNA content in BCL-XL-dependent H146 cells.
In vivo
Following a single 5 mg/kg IP dose of A-1155463 in nontumor bearing SCID-Beige mice, platelet counts fall dramatically as measured at 6 h postdose and then rebound to normal levels within 72 h. Daily Dosing at 5 mg/kg IP to SCID-Beige mice that had been inoculated with BCL-XL-dependent H146 tumor cells for 14 days causes a statistically significant inhibition of tumor growth (maximum tumor growth inhibition = 44%), which is alleviated upon cessation of dosing.
References
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