TNO155

Catalog No.S8987

For research use only.

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.

TNO155 Chemical Structure

CAS No. 1801765-04-7

Selleck's TNO155 has been cited by 1 Publication

Purity & Quality Control

Choose Selective phosphatase Inhibitors

Biological Activity

Description 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]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 421.95
Formula

C18H24ClN7OS

Density g/mL
CAS No. 1801765-04-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1C(C2(CCN(CC2)C3=CN=C(C(=N3)N)SC4=C(C(=NC=C4)N)Cl)CO1)N

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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.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04330664 Active not recruiting Drug: MRTX849|Drug: TNO155 Advanced Cancer|Metastatic Cancer|Malignant Neoplastic Disease Mirati Therapeutics Inc.|Novartis April 22 2020 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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