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SHP2-IN-13

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Catalog No. T78694Cas No. 2951854-02-5

SHP2-IN-13 is an orally active, highly selective allosteric inhibitor targeting the SHP2 "tunnel site," exhibiting an IC50 of 83.0 nM. It holds potential for research into cancers with RTK oncogenic drivers and diseases associated with SHP2.

SHP2-IN-13

SHP2-IN-13

😃Good
Catalog No. T78694Cas No. 2951854-02-5
SHP2-IN-13 is an orally active, highly selective allosteric inhibitor targeting the SHP2 "tunnel site," exhibiting an IC50 of 83.0 nM. It holds potential for research into cancers with RTK oncogenic drivers and diseases associated with SHP2.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$1,5206-8 weeks6-8 weeks
50 mg$1,9806-8 weeks6-8 weeks
100 mg$2,5006-8 weeks6-8 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Product Introduction

Bioactivity
Description
SHP2-IN-13 is an orally active, highly selective allosteric inhibitor targeting the SHP2 "tunnel site," exhibiting an IC50 of 83.0 nM. It holds potential for research into cancers with RTK oncogenic drivers and diseases associated with SHP2.
In vitro
SHP2-IN-13 (compound 129) effectively inhibits the pERK signaling pathway in a dose-dependent manner, with IC50 values of 0.59 μM in NSCLC cells and 0.63 ± 0.32 μM in NCI-H1975-OR cells [1]. At concentrations from 0 to 30 μM over 24 hours, it suppresses pERK levels and RTK-driven proliferation in NCI-H1975 cells and inhibits pERK levels in RTK-resistant NSCLC cells [1].
In vivo
In pharmacokinetic studies, SHP2-IN-13 (compound 129) (IV/PO; 5mg/kg) demonstrated high clearance, substantial volume of distribution (13.9 L/kg), and a moderate half-life (T 1/2 = 5.31 h), with oral bioavailability (F= 55.07±7.93%) exceeding that of SHP099 (F= 46%), making it suitable for further in vivo antitumor pharmacodynamic evaluation [1]. SHP2-IN-13 (oral gavage; 20 mg/kg; daily) exhibited potent anti-leukemic efficacy, which significantly reduced leukemic burden, and nearly eradicated CD45+ leukemic cells from human blood and spleen samples [1].
Chemical Properties
Molecular Weight327.38
FormulaC16H21N7O
Cas No.2951854-02-5
SmilesNC1=NC(=NC=C1C(NC=2C=CC=NC2)=O)N3CCC(C)(N)CC3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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