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BBP- 398 (IACS-13909) phosphatase inhibitor

Name: BBP- 398 (IACS-13909)
Brand: Selleck Chemicals
SKU: S9703
Rating: 5 (1 reviews)

Cat.No.S9703

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

Chemical Structure

Molecular Weight: 377.27

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other phosphatase Inhibitors	Osunprotafib (ABBV-CLS-484) SHP099 Hydrochloride RMC-4550 SHP099 GSK2830371 β-Glycerophosphate sodium salt hydrate Batoprotafib (TNO155) NSC87877 TPI-1 Sanguinarine chloride

Chemical Information, Storage & Stability

Molecular Weight	377.27	Formula	C₁₇H₁₈Cl₂N₆	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2160546-07-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (198.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (3.31mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (3.31mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	SHP2
In vitro	BBP-398 (IACS-13909) is a specific and potent allosteric inhibitor of SHP2 that suppresses signalling through the MAPK pathway. It potently impedes proliferation of tumours harbouring a broad spectrum of activated RTKs as the oncogenic driver, and this compound potently suppresses tumour cell proliferation in vitro.
In vivo	In EGFR-mutant osimertinib-resistant NSCLC models with EGFR-dependent and EGFR-independent resistance mechanisms, BBP-398 (IACS-13909) causes tumour regression in vivo when administered as a single agent or in combination with osimertinib.
References	[1] https://pubmed.ncbi.nlm.nih.gov/32928921/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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