TNO155

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TNO155 是一种蛋白酪氨酸磷酸酶 (PTP) 非受体 11 型 (SHP2; src 同源区 2 结构域磷酸酶; PTPN11) 抑制剂 (IC50 : 0.011 μM)，具有潜在的抗肿瘤活性。

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.

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.

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.

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Metabolic Enzyme/Protease

Phosphatase

SHP-2

Cancer

Advanced Cancer,Metastatic Cancer,Malignant Neoplastic Disease

1801765-04-7

421.95

C18H24ClN7OS

>98% (HPLC)

DMSO:185mg/ml (438.44 Mm; Need ultrasonic)

C[C@@H]1OCC2(CCN(CC2)C2=NC(N)=C(SC3=C(Cl)C(N)=NC=C3)N=C2)[C@@H]1N

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(-20℃)

With Ice Pack

≥ 2 years