2. Protein Tyrosine Kinase/RTK
  3. SHP2
  4. SHP2-IN-13

SHP2-IN-13 is a highly selective and orally active SHP2 “tunnel site” allosteric inhibitor with an IC50 of 83.0 nM. SHP2-IN-13 has the potential for cancers bearing RTK oncogenic drivers and SHP2-related diseases research.

For research use only. We do not sell to patients.

SHP2-IN-13 Chemical Structure

SHP2-IN-13 Chemical Structure

CAS No. : 2951854-02-5

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5 mg USD 340 In-stock
10 mg USD 550 In-stock
25 mg USD 1140 In-stock
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Based on 1 publication(s) in Google Scholar

SHP2-IN-13 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

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Description

SHP2-IN-13 is a highly selective and orally active SHP2 “tunnel site” allosteric inhibitor with an IC50 of 83.0 nM. SHP2-IN-13 has the potential for cancers bearing RTK oncogenic drivers and SHP2-related diseases research.

In Vitro

SHP2-IN-13 (compound 129) potently inhibits the pERK signaling in a dose-dependent manner with IC50 values of 0.59 μM and 0.63 ± 0.32 μM in NSCLC cells and NCI–H1975-OR cells, respectively.[1].
SHP2-IN-13 (0-30 μM; 24 hours) inhibited pERK levels and receptor tyrosine kinase (RTK)-driven cancer cell proliferation in NCI–H1975 cells, . And it also inhibits phosphorylated ERK (pERK) levels in receptor tyrosine kinase (RTK)-resistant NSCLC cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SHP2-IN-13 Related Antibodies

Western Blot Analysis[1]

Cell Line: NSCLC cells or NCI–H1975-OR cells
Concentration: 0 μM, 0.01 μM, 0.04 μM, 0.1 μM, 0.4 μM, 1.1 μM, 3.3 μM, 10 μM, 30 μM
Incubation Time: 24 hours
Result: Inhibited p-ERK expression in a dose-dependent manner.
In Vivo

In vivo pharmacokinetics studies, SHP2-IN-13 (compound 129) (IV/PO; 5mg/kg) demonstrates high clearance, a high volume of distribution (13.9 L/kg), a moderate half-life (T1/2=5.31 h). Additionally, SHP2-IN-13 shows a higher oral bioavailability (F =55.07 ± 7.93%) than SHP099 (F =46%) and is suitable for further in vivo anti-tumor evaluation[1].
SHP2-IN-13 (oral gavage; 20 mg/kg; daily) exhibits an anti-leukaemic efficacy and causes significant reduction of leukemia burden. Additionally, it near completely eradicated human CD45+ leukaemic cells in blood and spleen[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Murine NSG xenograft model inoculated with FLT3-ITD mutated MV-4-11-luciferase (MV-4-11-Luc) AML cells[1]
Dosage: 20 mg/kg
Administration: Oral gavage; 20 mg/kg; daily
Result: Exhibited an anti-tumour efficacy in AML model.
Molecular Weight

327.38

Formula

C16H21N7O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1(CCN(CC1)C2=NC=C(C(N)=N2)C(NC3=CN=CC=C3)=O)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (152.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0546 mL 15.2728 mL 30.5455 mL
5 mM 0.6109 mL 3.0546 mL 6.1091 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0546 mL 15.2728 mL 30.5455 mL 76.3639 mL
5 mM 0.6109 mL 3.0546 mL 6.1091 mL 15.2728 mL
10 mM 0.3055 mL 1.5273 mL 3.0546 mL 7.6364 mL
15 mM 0.2036 mL 1.0182 mL 2.0364 mL 5.0909 mL
20 mM 0.1527 mL 0.7636 mL 1.5273 mL 3.8182 mL
25 mM 0.1222 mL 0.6109 mL 1.2218 mL 3.0546 mL
30 mM 0.1018 mL 0.5091 mL 1.0182 mL 2.5455 mL
40 mM 0.0764 mL 0.3818 mL 0.7636 mL 1.9091 mL
50 mM 0.0611 mL 0.3055 mL 0.6109 mL 1.5273 mL
60 mM 0.0509 mL 0.2545 mL 0.5091 mL 1.2727 mL
80 mM 0.0382 mL 0.1909 mL 0.3818 mL 0.9545 mL
100 mM 0.0305 mL 0.1527 mL 0.3055 mL 0.7636 mL
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SHP2-IN-13 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SHP2-IN-132951854-02-5SHP2Src homology phosphatase 2PTPN11sHP2Receptor tyrosine kinaseLead compoundRTKoncogenicdriverSHP2-relateddiseasesAMLCANCERInhibitorinhibitorinhibit

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