IACS-13909

For research use only.

Catalog No.S9703 Synonyms: BBP-398

IACS-13909 Chemical Structure

CAS No. 2160546-07-4

IACS-13909 (BBP-398) is a specific and potent allosteric inhibitor of SHP2 (Src homology 2 domain-containing phosphatase) that suppresses signaling through the MAPK pathway.

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Choose Selective phosphatase Inhibitors

Biological Activity

Description IACS-13909 (BBP-398) is a specific and potent allosteric inhibitor of SHP2 (Src homology 2 domain-containing phosphatase) that suppresses signaling through the MAPK pathway.
Targets
SHP2 [1]
()
In vitro

IACS-13909 is a specific and potent allosteric inhibitor of SHP2 that suppresses signaling through the MAPK pathway. IACS-13909 potently impedes proliferation of tumors harboring a broad spectrum of activated RTKs as the oncogenic driver. IACS-13909 potently suppresses tumor cell proliferation in vitro.[1]

In vivo

In EGFR-mutant osimertinib-resistant NSCLC models with EGFR-dependent and EGFR-independent resistance mechanisms, IACS-13909, administered as a single agent or in combination with osimertinib, causes tumor regression in vivo.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: KYSE-520 cells
  • Concentrations: 0-10000 nM
  • Incubation Time: 2 h
  • Method:

    KYSE-520 cells are seeded (10,000 cells/40 µL/well) in 384-well tissue culture plates. The next day, cells are treated with DMSO or serially diluted IACS-13909 for 2 hours at 37℃, 5% CO2. Phospho-ERK levels are measured using AlphaScreen SureFire ERK1/2 (phospho‐Thr202/Tyr204) assay kit following manufacturer's recommendations. AlphaScreen signal is measured on an Envision plate reader using default AlphaScreen settings. Dose-response curves are analyzed using IC50 regression curve fitting.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: female CD1 mice; Sprague Dawley (SD) male rats; male adult beagle dogs
  • Dosages: 0.3 mg/kg, 10 mg/kg; 1 mg/kg, 3 mg/kg; 0.3 mg/kg, 1 mg/kg
  • Administration: IV, Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 75 mg/mL (198.79 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 377.27
Formula

C17H18Cl2N6

CAS No. 2160546-07-4
Storage powder
in solvent
Synonyms BBP-398

In vivo Formulation Calculator (Clear solution)

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04528836 Recruiting Drug: BBP-398 (Formerly Known as IACS-15509) Tumor Solid Navire Pharma Inc. a BridgeBio company November 12 2020 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID