Batoprotafib(TNO155)

Catalog No.S8987 Batch:S898701

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Technical Data

Formula

C18H24ClN7OS
Molecular Weight 421.95 CAS No. 1801765-04-7
Solubility (25°C)* In vitro DMSO 84 mg/mL (199.07 mM)
Ethanol 5 mg/mL (11.84 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.2mg/ml Taking the 1 mL working solution as an example, add 50 μL 84 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.)

Preparing Stock Solutions

Biological Activity

Description Batoprotafib(TNO155) is an inhibitor of protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2 /src homology region 2 domain phosphatase /PTPN11) with IC50 of 0.011 µM. TNO155 has potential antineoplastic activity.
Targets
SHP-2 [1]
(Cell-free assay)
0.011 μM
In vitro

TNO155 inhibits KYSE520 pERK and KYSE520 5-day cell proliferation with IC50 of 0.008 µM and of 0.100 µM, respectively. The off-target IC50 are 18 µM, 6.9 µM, 11 µM and > 30μM for Cav1.2, VMAT, SST3 and all others, respectively.[1]
In vivo

TNO155 is a potent and selective first-in-class inhibitor of wild-type SHP2, with high oral bioavailability and BCS class I properties. The oral bioavailability of TNO155 in mouse, rat and money are 78%, 86%, and 60%, respectively.[1]
Density g/mL

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    PC-14 cells

  • Concentrations

    3 μM

  • Incubation Time

    24 h

  • Method

    PC-14 cells were treated with nazartinib (0.1 or 0.3 µM), 3 µM TNO155, or the combination of nazartinib and TNO155 for 4 hours or 24 hours.

Selleck's Batoprotafib(TNO155) has been cited by 7 publications

Preclinical translational platform of neuroinflammatory disease biology relevant to neurodegenerative disease [ J Neuroinflammation, 2024, 21(1):37] PubMed: 38297405
Allosteric inhibitor of SHP2 enhances macrophage endocytosis and bacteria elimination by increasing caveolae activation and protects against bacterial sepsis [ Pharmacol Res, 2024, 201:107096] PubMed: 38320736
KRASG 12C-inhibitor-based combination therapies for pancreatic cancer: insights from drug screening [ Mol Oncol, 2024, 10.1002/1878-0261.13725] PubMed: 39253995
MUC1-C Is a Common Driver of Acquired Osimertinib Resistance in NSCLC [ J Thorac Oncol, 2023, 10.1016/j.jtho.2023.10.017] PubMed: 37924972
Mapping the landscape of genetic dependencies in chordoma [ Nat Commun, 2023, 14(1):1933] PubMed: 37024492
SHP2 deneddylation mediates tumor immunosuppression in colon cancer via the CD47/SIRPα axis [ J Clin Invest, 2023, 133(4)e162870] PubMed: 36626230
KRAS Secondary Mutations That Confer Acquired Resistance to KRAS G12C Inhibitors, Sotorasib and Adagrasib, and Overcoming Strategies: Insights From In Vitro Experiments [ J Thorac Oncol, 2021, 16(8):1321-1332] PubMed: 33971321

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.