An inhibitor of wild-type and mutant EGFR
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EGFR-IN-7

Item No. 42214

Technical Information
Formal Name
5-bromo-N4-[5-(dimethylphosphinyl)-6-quinoxalinyl]-N2-[2-methoxy-5-methyl-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-2,4-pyrimidinediamine
CAS Number
2267329-76-8
Synonyms
  • EGFR Inhibitor 7
  • Epidermal Growth Factor Receptor-IN-7
  • Epidermal Growth Factor Receptor Inhibitor 7
  • TQB3804
Molecular Formula
C32H41BrN9O2P
Formula Weight
Purity
≥95%
A solid
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
BrC1=CN=C(NC2=C(C=C(C(C)=C2)N3CCC(CC3)N4CCN(CC4)C)OC)N=C1NC5=CC=C(N=CC=N6)C6=C5P(C)(C)=O
InChi Code
InChI=1S/C32H41BrN9O2P/c1-21-18-26(28(44-3)19-27(21)42-12-8-22(9-13-42)41-16-14-40(2)15-17-41)38-32-36-20-23(33)31(39-32)37-25-7-6-24-29(35-11-10-34-24)30(25)45(4,5)43/h6-7,10-11,18-20,22H,8-9,12-17H2,1-5H3,(H2,36,37,38,39)
InChi Key
ZYSKXRAGBGLELB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    Product Description

    EGFR-IN-7 is an inhibitor of wild-type and mutant EGFR (IC50s = 1.07, 0.46, 0.13, 0.26, and 0.19 nM for wild-type EGFR, EGFRd746-750/T790M/C797S, EGFRL858R/T790M/C797S, EGFRd746-750/T790M, and EGFRL858R/T790M, respectively).1 It inhibits the proliferation of wild-type EGFR-expressing A431, EGFRd746-750/T790M/C797S-expressing Ba/F3, EGFRd746-750/T790M/C797S-expressing H1975, and EGFRd746-750-expressing PC-9 cells (IC50s = 147, 26.8, 163, and 45 nM, respectively). EGFR-IN-7 reduces tumor growth in triple mutant EGFR mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liu, X., Zhang, X., Yang, L., et alAbstract 1320: Preclinical evaluation of TQB3804, a potent EGFR C797S inhibitor. Cancer Res. 79(13_Suppl), (2019).