TNO155

SKU: orb1220096

Description

TNO155 is a protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2; src homology region 2 domain phosphatase; PTPN11) inhibitor(IC50 : 0.011 μM),with potential antineoplastic activity.

Key Properties

• CAS Number: 1801765-04-7
• MW: 421.95
• Purity: >98% (HPLC)
• Formula: C₁₈H₂₄ClN₇OS
• SMILES: C[C@@H]1OCC2(CCN(CC2)C2=NC(N)=C(SC3=C(Cl)C(N)=NC=C3)N=C2)[C@@H]1N
• Target: Phosphatase
• Solubility: DMSO:185mg/ml (438.44 Mm; Need ultrasonic)

Bioactivity

• In Vivo:
  Animal model: Female athymic nude mice bearing HT-29 xenografts. Dosage: 20 mg/kg alone or 10 mg/kg in combination with Dabrafenib and Trametinib. Administration: PO, twice daily for 40 days. Result: Resulted in moderate tumor growth inhibition. Maintained tumor stasis for more than 40 days when combined with Dabrafenib plus Trametinib.
• In Vitro:
  Cell Proliferation Assay Cell line: PC-9, PC-9 EGFRT790M/C797S, HCC827, HCC827-GR (gefinitib-resistant). Concentration: 0-1000 nM. Incubation time: 6 days. Result: Inhibited cell viability with IC50s of 1.56, 1.38, 0.77 and 1.38 μM against PC-9 and PC-9 EGFRT790M/C797S, HCC827 and HCC827-GR cells, respectively. Western blot analysis. Cell line: PC-14 (EGFRex19del). Concentration: 3 μM. Incubation time: 4h and 24 h. Result: Effectively reduced p-ERK levels at 4 hours but suffered a rebound at 24 hours.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Phosphatase