Theliatinib

CAS No. 1353644-70-8

Theliatinib( —— )

Catalog No. M20712 CAS No. 1353644-70-8

Theliatinib a potent and highly selective EGFR inhibitor with anti-tumor activity. Ki of 0.05 nM for wild type EGFR and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 164 In Stock
10MG 268 In Stock
25MG 442 In Stock
50MG 656 In Stock
100MG 888 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    Theliatinib
  • Note
    Research use only, not for human use.
  • Brief Description
    Theliatinib a potent and highly selective EGFR inhibitor with anti-tumor activity. Ki of 0.05 nM for wild type EGFR and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant respectively.
  • Description
    Theliatinib a potent and highly selective EGFR inhibitor with anti-tumor activity. Ki of 0.05 nM for wild type EGFR and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant respectively.(In Vivo):Theliatinib (2-15 mg/kg; oral administration;daily; for 21 days; NOD-SCID mice; PDECX 1T0950 model) treatment demonstrates tumor regression of 75% at the end of study, and with a dose response.
  • In Vitro
    ——
  • In Vivo
    Theliatinib (2-15 mg/kg; oral administration;daily; for 21 days; NOD-SCID mice; PDECX 1T0950 model) treatment demonstrates tumor regression of75% at the end of study, and with a dose response. Animal Model:NOD-SCID mice injected with esophageal cancer cells (PDECX 1T0950 model)Dosage:2 mg/kg, 5 mg/kg, 15 mg/kg Administration:Oral administration;daily; for 21 days Result:Attenuated tumor growth in PDECX 1T0950 model in a dose-dependent manner.
  • Synonyms
    ——
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    EGFR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1353644-70-8
  • Formula Weight
    442.5
  • Molecular Formula
    C25H26N6O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:47 mg/mL (106.21 mM)
  • SMILES
    [H][C@]12CCN(C)[C@@]1([H])CN(C2)C(=O)Nc1cc2c(Nc3cccc(c3)C#C)ncnc2cc1OC
  • Chemical Name
    (3aR6aR)-N-(4-((3-ethynylphenyl)amino)-7-methoxyquinazolin-6-yl)-1-methylhexahydropyrrolo[34-b]pyrrole-5(1H)-carboxamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Ren Y Zheng J Fan S et al. Anti-tumor efficacy of theliatinib in esophageal cancer patient-derived xenografts models with epidermal growth factor receptor (EGFR) overexpression and gene amplification.[J]. Oncotarget 2017 8(31):50832-50844.
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