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Batoprotafib (TNO155) SHP2 inhibitor

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.
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Quality Control

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

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

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In vivo
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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.

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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

Synonyms N/A SMILES CC1C(C2(CCN(CC2)C3=CN=C(C(=N3)N)SC4=C(C(=NC=C4)N)Cl)CO1)N

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Mechanism of Action

Targets/IC50/Ki
SHP-2
(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.

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.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-09-04)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07468071 RECRUITING
Locally Advanced or Metastatic KRAS G12C-mutated Non-small Cell Lung Cancer; Advanced Solid Tumors Harboring the KRAS G12C Mutation
Novartis Pharmaceuticals
2026-06-08 PHASE1; PHASE2
NCT04699188 ACTIVE_NOT_RECRUITING
KRAS G12C Mutant Solid Tumors; Carcinoma, Non-Small-Cell Lung; Carcinoma, Colorectal; Cancer of Lung; Cancer of the Lung; Lung Cancer; Neoplasms, Lung; Neoplasms, Pulmonary; Pulmonary Cancer; Pulmonary Neoplasms
Novartis Pharmaceuticals
2021-02-24 PHASE1; PHASE2
NCT04185883 ACTIVE_NOT_RECRUITING
Advanced Solid Tumors; Kirsten Rat Sarcoma (KRAS) pG12C Mutation
Amgen
2019-12-17 PHASE1
NCT05541159 WITHDRAWN
Renal Impairment
Novartis Pharmaceuticals
2025-03-19 PHASE1
NCT03114319 TERMINATED
Advanced EGFR Mutant Non Small Cell LungCancer (NSCLC); KRAS G12-mutant NSCLC; Esophageal Squamous Cell Cancer (SCC); Head/Neck SCC; Melanoma; Advanced Gastrointestinal Stromal Tumors (GIST); Advanced NRAS/BRAFT wt Cutaneous Melanoma
Novartis Pharmaceuticals
2017-05-26 PHASE1
NCT05490030 WITHDRAWN
Hepatic Impairment
Novartis Pharmaceuticals
2025-03-06 PHASE1

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