1398833-56-1

1398833-56-1 structure
1398833-56-1 structure
  • Name: NT-113
  • Chemical Name: NT113
  • CAS Number: 1398833-56-1
  • Molecular Formula:
  • Molecular Weight:
  • Catalog: Research Areas Cancer
  • Create Date: 2018-06-07 05:47:40
  • Modify Date: 2024-01-02 11:53:25
  • NT-113 is an irreversible pan-ERBB inhibitor, with IC50s of 0.4, 4.35, 4.18 and 2.08 nM for EGFR, EGFRT790M, ERBB2/HER2 and ERBB4/HER4, respectively, exhibiting anti-glioma activities.

Name NT113
Synonyms NT-113
Description NT-113 is an irreversible pan-ERBB inhibitor, with IC50s of 0.4, 4.35, 4.18 and 2.08 nM for EGFR, EGFRT790M, ERBB2/HER2 and ERBB4/HER4, respectively, exhibiting anti-glioma activities.
Related Catalog
Target

EGFR:0.4 nM (IC50)

ErbB2:4.18 nM (IC50)

ErbB4:2.08 nM (IC50)

EGFRT790M:4.35 nM (IC50)

In Vitro NT113 shows inhibitory activity against U87vIII cells, with IC50 of 0.19 μM[1].
In Vivo NT113 (20 mg/kg/day) shows inhibitory activity against intracranial EGFRvIII-amplified GBM39 xenograft tumors. NT113 (10 mg/kg/day) causes growth delay in the U87vIII intracranial xenografts. Mice receiving NT113 treatment survive significantly longer than mice receiving lapatinib[1].
Cell Assay Cells are seeded in 96 well plates: 2000 cells/well in 200 μL, in hextuplicate. One day after seeding, 1 μL of DMSO, with or without NT113, is added to cells to achieve NT113 concentrations between 0.01 and 20.0 μM. Seventy-two hours later, WST-1 reagent is added, and sample 450 nm absorbance determined using a microplate reader, with background reading at 800 nm subtracted.
Animal Admin Mice with intracranial GBM12 tumors are administered NT113, at 10 mg/kg/day for 3 days, with blood and intracranial tissue samples obtained 2 hours following the third administration. Plasma is separated from whole blood, and frozen at −80°C. After brain resection, tumor tissue is immediately dissected from tumor-bearing hemisphere, then snap frozen and stored at −80°C, as is contralateral hemisphere without tumor. NT113 is extracted from homogenized tissues using a Bullet Blender. Homogenates are extracted with organic solvent and further processed prior to transfer to an autosampler for high performance liquid chromatography (HPLC) analysis, and determination of NT113 content.
References

[1]. Yoshida Y, et al. NT113, a pan-ERBB inhibitor with high brain penetrance, inhibits the growth of glioblastoma xenografts with EGFR amplification. Mol Cancer Ther. 2014 Dec;13(12):2919-29

No Any Chemical & Physical Properties