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AT13148

Technical Data

Molecular Weight 313.78 Storage powder
Formula

C17H16ClN3O

in solvent
CAS No. 1056901-62-2 Synonyms N/A
Chemical Name (S)-1-(4-(1H-pyrazol-4-yl)phenyl)-2-amino-1-(4-chlorophenyl)ethanol
Solubility (25°C) * In vitro DMSO 62 mg/mL (197.59 mM)
Water Insoluble
Ethanol Insoluble
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Biological Activity

Description AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.
Targets
PKA [1]
(Cell-free assay)
ROCK2 [1]
(Cell-free assay)
ROCK1 [1]
(Cell-free assay)
p70S6K [1]
(Cell-free assay)
Akt1 [1]
(Cell-free assay)
3 nM 4 nM 6 nM 8 nM 38 nM
In vitro AT13148, as a multi-AGC kinase inhibitor, potently inhibits proliferation with GI50 values of 1.5 to 3.8 μM across a selected panel of cancer cell lines with deregulation of PI3K-AKT-mTOR or RAS-RAF pathways. In PTEN-deficient MES-SA cells, AT13148 also inhibits AKT and p70S6K signaling. [1]
In vivo AT13148 (50 mg/kg p.o.) markedly inhibits the activity of both AKT and p70S6K AGC kinases, and subsequently exhibits marked antitumor effects in human tumor xenografts. [1]
Features  

Protocol (Only for Reference)

Kinase Assay:

[1]

In vitro kinase assays AT13148 is assayed against 40 kinases and the percentage inhibition at 10 μM of AT13148 is determined. Individual IC50 values are measured for selected kinases using ATP concentrations equivalent to the Km for each enzyme.
Cell Assay:

[1]

Cell lines MES-SA, MES-SA/Dx5, BT474, HCT-116, A549, PC3, SK-BR-3, MCF7, U87MG, MDA-MB-468, DU-145, and SK-OV-3 cell lines
Concentrations ~10 μM
Incubation Time 72 hours or 96 hours
Method

Cytotoxicity is determined using a 72 h Alamar Blue assay or a 96 h SRB assay.

Animal Study:

[1]

Animal Models Athymic mice bearing MES-SA, BT474, or PC3 tumor xenografts
Formulation 10% DMSO, 1% Tween-20, and 89% saline
Dosages ~50 mg/kg
Administration p.o.
 

References:

Customer Product Validation

Data from [Data independently produced by , , Biochem Biophys Res Commun, 2016, 478(1):330-6.]

AT13148 exerts cytotoxic and anti-proliferative activity against human gastric cancer cells. Human gastric cancer cells (HGC-27, AGS, SNU-601, N87 and MKN-28 lines) or GEC-1 gastric epithelial cells were treated with applied concentration of AT13148 for indicated time, cell survival (A and E), cell proliferation (B and F), cell cycle distribution (C, for HGC-27 cells) and cell death (D, for HGC-27 cells) were tested by the described assays, separately. Data were presented as mean ± SD. “Ctrl” stands for untreated control cells (For all figures). “hr/hrs” stands for hour/hours (For all figures). Experiments in this figure were repeated for five times. *p < 0.05 vs. “Ctrl” group.

AT13148 has been referenced in publications.

PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products are stable under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage temperature. Short-term storage of many products are stable in the short-term at temperatures that differ from that required for long-term storage.
We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, follow the storage recommendations on the product data sheet.

Chemical Structure

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