[CAS NO. 1235034-55-5]  A-1155463

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PRODUCTS SPECIFICATIONS [1235034-55-5]

Catelog
SLK-S7800
Brand
Selleck
CAS
1235034-55-5

DESCRIPTION [1235034-55-5]

Overview

MDLMFCD29924714
Molecular Weight669.79
Molecular FormulaC35H32FN5O4S2
SMILESO=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

Shipping

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

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.4930 mL7.4650 mL14.9301 mL
5 mM0.2986 mL1.4930 mL2.9860 mL
10 mM0.1493 mL0.7465 mL1.4930 mL
50 mM0.0299 mL0.1493 mL0.2986 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.