Home Metabolism phosphatase inhibitor BBP- 398 (IACS-13909) For research use only.

BBP- 398 (IACS-13909)

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.

BBP- 398 (IACS-13909) Chemical Structure

BBP- 398 (IACS-13909) Chemical Structure

CAS No. 2160546-07-4

Purity & Quality Control

BBP- 398 (IACS-13909) Related Products

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
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]
Cell Research 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.
In Vivo
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]
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05621525 Recruiting
Advanced Solid Tumor|Advanced or Metastatic Non-small Cell Lung Cancer
LianBio LLC
 October 18 2022 Phase 1
NCT05375084 Recruiting
Non Small Cell Lung Cancer|Solid Tumor
Navire Pharma Inc. a BridgeBio company|Bristol-Myers Squibb
 October 20 2022 Phase 1
NCT05480865 Recruiting
Solid Tumor Adult|Metastatic Solid Tumor|Metastatic NSCLC|Non Small Cell Lung Cancer
Navire Pharma Inc. a BridgeBio company|Amgen
 July 6 2022 Phase 1
NCT04528836 Active not recruiting
Tumor Solid
Navire Pharma Inc. a BridgeBio company
 November 12 2020 Phase 1

Chemical Information & Solubility

Molecular Weight 377.27 Formula

C17H18Cl2N6
CAS No. 2160546-07-4 SDF --
Smiles CC1(N)CCN(CC1)C2=CN=C3C(=N2)[NH]N=C3C4=CC=CC(=C4Cl)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 75 mg/mL ( (198.79 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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