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A-1155463

Catalog No. T6748   CAS 1235034-55-5
Synonyms: A 1155463, A1155463

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).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
A-1155463 Chemical Structure
A-1155463, CAS 1235034-55-5
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
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1 mL * 10 mM (in DMSO) In stock $ 132.00
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Purity: 99%
Purity: 98%
Purity: 96.1%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (149.3 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 100 mg/mL (149.3 mM)

TargetMolReferences and Literature

1. Tao ZF, et al. ACS Med Chem Lett. 2014, 5(10):1088-93. 2. Leverson JD, et al. Sci Transl Med. 2015, 7(279):279ra40. 3. Haichao Zhang, et al. Molecular Cancer. 2015, 14(1):1-9.

TargetMolCitations

1. Devin J, Cañeque T, Lin Y L, et al. Targeting cellular iron homeostasis with ironomycin in diffuse large B cell lymphoma. Cancer Research. 2022 2. Devin J, Cañeque T, Lin Y L, et al. Targeting cellular iron homeostasis with ironomycin in diffuse large B cell lymphomaTargeting cellular iron homeostasis with ironomycin in DLBCL. Cancer Research. 2022

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Bioactive Compound Library Mitochondria-Targeted Compound Library Anti-COVID-19 Compound Library Inhibitor Library Anti-Aging Compound Library NO PAINS Compound Library Anti-Cancer Compound Library Cuproptosis Compound Library Bioactive Compounds Library Max

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Keywords

A-1155463 1235034-55-5 Apoptosis BCL Bcl-2 Family Inhibitor A 1155463 A1155463 inhibit inhibitor

 

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