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A 410099.1

Cat. No. 6470 1 Citation Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: High affinity XIAP antagonist; active in vivo
Chemical Name: N-Methyl-L-alanyl-(2S)-2-cyclohexylglycyl-N-[(1R)-1,2,3,4-tetrahydro-1-naphthalenyl]-L-prolinamide hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (1)
Pathways (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for A 410099.1

A 410099.1 is a high affinity XIAP antagonist (Kd = 16 nM for the BIR3 domain of XIAP). Exhibits cytotoxicity in a wide range of cancer cell lines in vitro (EC50 = 13 nM in MDA-MB-231 cells). Also displays antitumor activity in a mouse breast cancer xenograft model. Enhances TRAIL-induced apoptosis in chronic lymphocytic leukemia (CLL) cells.

Compound Libraries for A 410099.1

A 410099.1 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for A 410099.1

M. Wt 505.09
Formula C27H40N4O3.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 762274-58-8
PubChem ID 131858992
InChI Key OPCYOBWCDDJCFT-VOSOYEAFSA-N
Smiles CN[C@H](C(N[C@H](C(N1CCC[C@H]1C(N[C@@H]2CCCC3=CC=CC=C23)=O)=O)C4CCCCC4)=O)C.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for A 410099.1

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 50.51 100
DMSO 50.51 100

Preparing Stock Solutions for A 410099.1

The following data is based on the product molecular weight 505.09. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.98 mL 9.9 mL 19.8 mL
5 mM 0.4 mL 1.98 mL 3.96 mL
10 mM 0.2 mL 0.99 mL 1.98 mL
50 mM 0.04 mL 0.2 mL 0.4 mL

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References for A 410099.1

References are publications that support the biological activity of the product.

Oost et al (2004) Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer. J.Med.Chem. 47 4417 PMID: 15317454

Loeder et al (2009) A novel paradigm to trigger apoptosis in chronic lymphocytic leukemia. Cancer Res. 69 8977 PMID: 19920200

If you know of a relevant reference for A 410099.1, please let us know.

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Keywords: A 410099.1, A 410099.1 supplier, A410099.1, A4100991, XIAP, antagonists, antagonism, inhibitors, inhibits, high, affinity, x-linked, inhibitor, of, apoptosis, IAP, anticancer, Inhibitor, Apoptosis, (IAP), 6470, Tocris Bioscience

1 Citation for A 410099.1

Citations are publications that use Tocris products. Selected citations for A 410099.1 include:

Susanne et al (2022) A Toolbox for the Generation of Chemical Probes for Baculovirus IAP Repeat Containing Proteins. Front Cell Dev Biol 10 886537 PMID: 35721509

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Literature in this Area

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Programmed Cell Death Poster

Programmed Cell Death Poster

There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.

Pathways for A 410099.1

Apoptosis Signaling Pathway

Apoptosis Signaling Pathway

Apoptosis is a physiological process for cell death that is critical during aging and development. It may also be referred to as cell 'suicide'. Apoptosis can be triggered by events both inside and outside of the cell.