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Batoprotafib (TNO155) SHP2 inhibitor

Name: Batoprotafib (TNO155)
Brand: Selleck Chemicals
SKU: S8987
Availability: InStock
Rating: 5 (9 reviews)

Cat.No.S8987

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, and has potential antineoplastic activity.

Chemical Structure

Molecular Weight: 421.95

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S898701 DMSO]84 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false Purity: 99.44%

99.44

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE PPAR HSP (HSP90) Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Amino Acids and Derivatives Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO Hydroxylase PCSK9 OXPHOS ROR
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Chemical Information, Storage & Stability

Molecular Weight	421.95	Formula	C₁₈H₂₄ClN₇OS	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1801765-04-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1C(C2(CCN(CC2)C3=CN=C(C(=N3)N)SC4=C(C(=NC=C4)N)Cl)CO1)N

Solubility

In vitro
Batch:

DMSO : 84 mg/mL (199.07 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : 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.
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.	4.200mg/ml (9.95mM)	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.

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	SHP-2 ^[1] (Cell-free assay) 0.011 μM
In vitro	Batoprotafib (TNO155) inhibits KYSE520 pERK and KYSE520 5-day cell proliferation with IC50 of 0.008 µM and of 0.100 µM, respectively. Its 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	Batoprotafib (TNO155) is a potent and selective first-in-class inhibitor of wild-type SHP2, with high oral bioavailability and BCS class I properties. Its oral bioavailability in mouse, rat and monkey are 78%, 86%, and 60%, respectively.^[1]
References	[1] https://colectivogist.files.wordpress.com/2017/11/nuevos-ensayos-geis-2017.pdf [2] https://pubmed.ncbi.nlm.nih.gov/33046519/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05541159	Withdrawn	Renal Impairment	Novartis Pharmaceuticals\|Pharmaceutical Research Associates\|Novartis	March 19 2025	Phase 1
NCT05490030	Withdrawn	Hepatic Impairment	Novartis Pharmaceuticals\|Pharmaceutical Research Associates\|Novartis	March 6 2025	Phase 1
NCT04330664	Active not recruiting	Advanced Cancer\|Metastatic Cancer\|Malignant Neoplastic Disease	Mirati Therapeutics Inc.\|Novartis	April 22 2020	Phase 1\|Phase 2

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