BBP- 398 (IACS-13909)

Catalog No.S9703 Batch:S970301

Print

Technical Data

Formula

C17H18Cl2N6

Molecular Weight 377.27 CAS No. 2160546-07-4
Solubility (25°C)* In vitro DMSO 75 mg/mL (198.79 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.)

Preparing Stock Solutions

Biological Activity

Description BBP- 398 (IACS-13909) 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 (from reference)

Cell Assay:

[1]

  • 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.

Animal Study:

[1]

  • 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

Selleck's BBP- 398 (IACS-13909) has been cited by 1 publication

Preclinical translational platform of neuroinflammatory disease biology relevant to neurodegenerative disease [ J Neuroinflammation, 2024, 21(1):37] PubMed: 38297405

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.