AT13148

Catalog No.S7563 Batch:S756301

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Technical Data

Formula

C17H16ClN3O
Molecular Weight 313.78 CAS No. 1056901-62-2
Solubility (25°C)* In vitro DMSO 62 mg/mL (197.59 mM)
Water Insoluble
Ethanol Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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)		 View More
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]

Protocol (from 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

  • Dosages

    ~50 mg/kg

  • Administration

    p.o.

Customer Product Validation

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

Selleck's AT13148 has been cited by 13 publications

Therapeutic targeting of tumor spheroids in a 3D microphysiological renal cell carcinoma-on-a-chip system [ Neoplasia, 2023, 10.1016/j.neo.2023.100948] PubMed: 37944353
Immunogenic Death of Hepatocellular Carcinoma Cells in Mice Expressing Caspase-Resistant ROCK1 Is Not Replicated by ROCK Inhibitors [ Cancers (Basel), 2022, 14(23)5943] PubMed: 36497425
A preclinical pipeline to evaluate migrastatics as therapeutic agents in metastatic melanoma [ Br J Cancer, 2021, 10.1038/s41416-021-01442-6] PubMed: 34172930
DAPL1 is a novel regulator of testosterone production in Leydig cells of mouse testis [ Sci Rep, 2021, 11(1):18532] PubMed: 34535743
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] PubMed: 32645325
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] PubMed: 32645325
Myosin II Reactivation and Cytoskeletal Remodeling as a Hallmark and a Vulnerability in Melanoma Therapy Resistance. [ Cancer Cell, 2020, 37(1):85-103] PubMed: 31935375
MKI-1, a Novel Small-Molecule Inhibitor of MASTL, Exerts Antitumor and Radiosensitizer Activities Through PP2A Activation in Breast Cancer [ Front Oncol, 2020, 10:571601] PubMed: 33117702
Mapping phospho-catalytic dependencies of therapy-resistant tumours reveals actionable vulnerabilities. [ Nat Cell Biol, 2019, 21(6):778-790] PubMed: 31160710
LncRNA HAND2-AS1 overexpression inhibits cancer cell proliferation in melanoma by downregulating ROCK1. [ Oncol Lett, 2019, 18(2):1005-1010] PubMed: 31423160

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.