Powder: -20°C for 3 years | In solvent: -80°C for 1 year
A-1155463, a highly potent and selective BCL-XL 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).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 38.00 | |
2 mg | In stock | $ 54.00 | |
5 mg | In stock | $ 89.00 | |
10 mg | In stock | $ 147.00 | |
25 mg | In stock | $ 275.00 | |
50 mg | In stock | Inquiry | |
1 mL * 10 mM (in DMSO) | In stock | $ 132.00 |
Description | A-1155463, a highly potent and selective BCL-XL 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&IC50 | Bcl-xL:<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[2]. |
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[1]. |
Kinase Assay | Recombinant p38 isoforms are activated by Mkk6(E) under the following conditions: p38 (100 ng/mL), Mkk6(E) (30 ng/mL), ATP (100 mM) are mixed in kinase buffer (25 mM Hepes, 25 mM b-glycerophosphate, 0.1 mM sodium orthovanadate, 25 mM MgCl2, 2.5 mM DTT, pH 7.4) and incubated for 30 min at 30°C. A typical assay reaction for Mnk1 activity contained Mnk1 (2 ng/mL), HA-eIF4E (10 ng/mL), ATP (300 mM) in kinase buffer. The reaction is started by addition of activated p38 (0.03-3 ng/mL) and stopped after 30 min at 30°C by addition of SDS loading buffer. Inhibitors of Mnk1 are identified under the same assay conditions, except that Mnk1 is pre-activated using active p38a before exposure to the substrate and inhibitors. |
Cell Research | Cells are treated with increasing concentration of A-1155463. Cells are assayed for viability after 72 h using the CellTiter-Glo luminescent cell viability assay according to the manufacturer's protocol. Results are normalized to cells without treatment. EC50 is calculated using the GraphPad Prism software.(Only for Reference) |
Animal Research | Animal Models: SCID-Beige MiceFormulation: 5% DMSO, 10% EtOH, 20% Cremaphor ELP, and 65% D5WDosages: 5 mg/kgAdministration: i.p. |
Synonyms | A 1155463, A1155463 |
Molecular Weight | 669.79 |
Formula | C35H32FN5O4S2 |
CAS No. | 1235034-55-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (149.3 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 100 mg/mL (149.3 mM)
You can also refer to dose conversion for different animals. More
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A-1155463 1235034-55-5 Apoptosis BCL Bcl-2 Family Inhibitor A 1155463 A1155463 inhibit inhibitor