BBP- 398 (IACS-13909)

Catalog No.S9703 Batch:S970301

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.)

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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

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

References

[1] Yuting Sun, et al. Cancer Res. 2020 Nov 1;80(21):4840-4853.

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

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

PubMed: 38297405

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